A new synthetic route of 2-(Bromoacetyl)pyridine hydrobromide

The synthetic route of 17570-98-8 has been constantly updated, and we look forward to future research findings.

Reference of 17570-98-8 , The common heterocyclic compound, 17570-98-8, name is 2-(Bromoacetyl)pyridine hydrobromide, molecular formula is C7H7Br2NO, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc., below Introduce a new synthetic route.

Example 6; 1 -(4-(1 -f6-methylpyridin-3-yl)-4-(pyridin-2-vO-1 H-imidazol-2-yltohenyl)-1 H-pyrrolor2.3- bipyridi?e; A mechanically stirred suspension of N’-(6-methylpyridin-3-yl)-4-(1H-pyrrolo[2,3- b]pyridin-1-yl)benzamidine (49.6 g, 152 mmol) in anhydrous THF (1 L) was treated over 30 mi? at less than 40C with a solution of LiHMDS (350 mL of 1M in THF). After 15 mi? at 0 0C the clear brown solution was treated portionwise at 3-6 0C with 2-bromo-1-(pyridin-2- yl)ethanone hydrobromide (42.6 g, 152 mmol) over 20 min. After being stirred 30 min at 00C and the mixture was warmed to 25 0C over 1h and stirred at 25 0C for 30 min. Water (500 mL) and EtOAc (1L) were added and the organic layer was separated, washed with brine, dried over Na2SO4, and concentrated. The residue was dissolved in 200 mL acetic acid and the resulting solution heated at 95 0C for 20 min and concentrated. The residue was dissolved in EtOAc (1L) and 2N HCI (450 mL). The organic layer was separated and washed with water (150 mL) and aqueous 10% citric acid (250 mL). The citric acid layer was extracted with EtOAc (2 x 100 mL). The combined organic layers were washed with water, brine, dried, and concentrated giving 42 g of crude product as a brown oil which was purified by SGC (1% MeOH in DCM, 0.5 % NH4OH), giving the title substance in several fractions contaminated with 1-7% of the corresponding amide <4-(1H-pyrrolo[2,3-b]pyridin-1- yl)benzamide) as determined by HPLC (280 nM absorption ratio). Yield 15 g, 31%. The material was efficiently further purified by recrystallization as illustrated: a 4.5 g fraction containing 3.5% amide impurity was dissolved in 98:2 acetonitrile:water and the resulting solution stirred at RT fro 40 min. The crystalline precipitate was filtered, washed with fresh acetonitrile and dried giving 2.9 g of the title substance containing 0.3% amide. In this manner the remaining fractions were purified and the recrystallized solids combined giving 9.35 g of the title substance containing less than 1% amide impurity. 1H NMR (CDCI3) delta 8.58 (m, 2H), 8.37 (dd, 1H, J = 1.5, 4.8 Hz), 8.16 (d, 1H1 J = 7.9 Hz)1 7.97 (dd, 1H, J = 1.7, 7.9 Hz), 7.91 (br, 1H)1 7.82 (m, 2H)1 7.79 (td, 1H1 J = 1.7, 7.9 Hz), 7.62 (m, 2H)1 7.53-7.50 (m, 2H)1 7.24-7.19 (m, 2H), 7.15 (dd, 1H, J = 4.6. 7.9 Hz), 6.65 (d, 1 H, J = 3.7 Hz), 2.64 (s, 3H). MS (AP+) m/e 429 (MH+). Anal. Calcd for C27H20N6: C1 75.68; H1 4.70; N1 19.61. Found: C1 75.39; H1 4.52; N1 19.64. ICs0 = <3.21 nM The synthetic route of 17570-98-8 has been constantly updated, and we look forward to future research findings. Reference:
Patent; PFIZER PRODUCTS INC.; WO2008/4117; (2008); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Some scientific research about 17570-98-8

According to the analysis of related databases, 17570-98-8, the application of this compound in the production field has become more and more popular.

Application of 17570-98-8, As we all know, there are many different methods for the synthesis of a compound, and people can choose the synthesis method that suits their own laboratory according to the actual situation. 17570-98-8, name is 2-(Bromoacetyl)pyridine hydrobromide, molecular formula is C7H7Br2NO, The compound is widely used in many fields, so it is necessary to find a new synthetic route. The downstream synthesis method of this compound is introduced below.

General procedure: 5.1.1 General procedure A (for synthesis of compounds 1-19). To 2-bromoacetylpyridine hydrobromide (1.0 equiv) in anhydrous ethanol (5 mL) was added the corresponding thiourea (1.0 equiv, 0.2 g) and the reaction mixture refluxed for 4 h. After cooling to ambient temperature the reaction mixture was poured into water. The pH of the mixture was adjusted to pH 8 with concentrated aqueous NH4OH and the mixture stirred for 2 h. The precipitate was filtered, washed with ethanol and dried to afford the title compound.

According to the analysis of related databases, 17570-98-8, the application of this compound in the production field has become more and more popular.

Reference:
Article; Meissner, Anja; Boshoff, Helena I.; Vasan, Mahalakshmi; Duckworth, Benjamin P.; Barry III, Clifton E.; Aldrich, Courtney C.; Bioorganic and Medicinal Chemistry; vol. 21; 21; (2013); p. 6385 – 6397;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

A new synthetic route of 2-(Bromoacetyl)pyridine hydrobromide

The synthetic route of 17570-98-8 has been constantly updated, and we look forward to future research findings.

Reference of 17570-98-8 , The common heterocyclic compound, 17570-98-8, name is 2-(Bromoacetyl)pyridine hydrobromide, molecular formula is C7H7Br2NO, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc., below Introduce a new synthetic route.

Example 6; 1 -(4-(1 -f6-methylpyridin-3-yl)-4-(pyridin-2-vO-1 H-imidazol-2-yltohenyl)-1 H-pyrrolor2.3- bipyridi?e; A mechanically stirred suspension of N’-(6-methylpyridin-3-yl)-4-(1H-pyrrolo[2,3- b]pyridin-1-yl)benzamidine (49.6 g, 152 mmol) in anhydrous THF (1 L) was treated over 30 mi? at less than 40C with a solution of LiHMDS (350 mL of 1M in THF). After 15 mi? at 0 0C the clear brown solution was treated portionwise at 3-6 0C with 2-bromo-1-(pyridin-2- yl)ethanone hydrobromide (42.6 g, 152 mmol) over 20 min. After being stirred 30 min at 00C and the mixture was warmed to 25 0C over 1h and stirred at 25 0C for 30 min. Water (500 mL) and EtOAc (1L) were added and the organic layer was separated, washed with brine, dried over Na2SO4, and concentrated. The residue was dissolved in 200 mL acetic acid and the resulting solution heated at 95 0C for 20 min and concentrated. The residue was dissolved in EtOAc (1L) and 2N HCI (450 mL). The organic layer was separated and washed with water (150 mL) and aqueous 10% citric acid (250 mL). The citric acid layer was extracted with EtOAc (2 x 100 mL). The combined organic layers were washed with water, brine, dried, and concentrated giving 42 g of crude product as a brown oil which was purified by SGC (1% MeOH in DCM, 0.5 % NH4OH), giving the title substance in several fractions contaminated with 1-7% of the corresponding amide <4-(1H-pyrrolo[2,3-b]pyridin-1- yl)benzamide) as determined by HPLC (280 nM absorption ratio). Yield 15 g, 31%. The material was efficiently further purified by recrystallization as illustrated: a 4.5 g fraction containing 3.5% amide impurity was dissolved in 98:2 acetonitrile:water and the resulting solution stirred at RT fro 40 min. The crystalline precipitate was filtered, washed with fresh acetonitrile and dried giving 2.9 g of the title substance containing 0.3% amide. In this manner the remaining fractions were purified and the recrystallized solids combined giving 9.35 g of the title substance containing less than 1% amide impurity. 1H NMR (CDCI3) delta 8.58 (m, 2H), 8.37 (dd, 1H, J = 1.5, 4.8 Hz), 8.16 (d, 1H1 J = 7.9 Hz)1 7.97 (dd, 1H, J = 1.7, 7.9 Hz), 7.91 (br, 1H)1 7.82 (m, 2H)1 7.79 (td, 1H1 J = 1.7, 7.9 Hz), 7.62 (m, 2H)1 7.53-7.50 (m, 2H)1 7.24-7.19 (m, 2H), 7.15 (dd, 1H, J = 4.6. 7.9 Hz), 6.65 (d, 1 H, J = 3.7 Hz), 2.64 (s, 3H). MS (AP+) m/e 429 (MH+). Anal. Calcd for C27H20N6: C1 75.68; H1 4.70; N1 19.61. Found: C1 75.39; H1 4.52; N1 19.64. ICs0 = <3.21 nM The synthetic route of 17570-98-8 has been constantly updated, and we look forward to future research findings. Reference:
Patent; PFIZER PRODUCTS INC.; WO2008/4117; (2008); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Some scientific research about 17570-98-8

According to the analysis of related databases, 17570-98-8, the application of this compound in the production field has become more and more popular.

Application of 17570-98-8, As we all know, there are many different methods for the synthesis of a compound, and people can choose the synthesis method that suits their own laboratory according to the actual situation. 17570-98-8, name is 2-(Bromoacetyl)pyridine hydrobromide, molecular formula is C7H7Br2NO, The compound is widely used in many fields, so it is necessary to find a new synthetic route. The downstream synthesis method of this compound is introduced below.

General procedure: 5.1.1 General procedure A (for synthesis of compounds 1-19). To 2-bromoacetylpyridine hydrobromide (1.0 equiv) in anhydrous ethanol (5 mL) was added the corresponding thiourea (1.0 equiv, 0.2 g) and the reaction mixture refluxed for 4 h. After cooling to ambient temperature the reaction mixture was poured into water. The pH of the mixture was adjusted to pH 8 with concentrated aqueous NH4OH and the mixture stirred for 2 h. The precipitate was filtered, washed with ethanol and dried to afford the title compound.

According to the analysis of related databases, 17570-98-8, the application of this compound in the production field has become more and more popular.

Reference:
Article; Meissner, Anja; Boshoff, Helena I.; Vasan, Mahalakshmi; Duckworth, Benjamin P.; Barry III, Clifton E.; Aldrich, Courtney C.; Bioorganic and Medicinal Chemistry; vol. 21; 21; (2013); p. 6385 – 6397;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Brief introduction of 17570-98-8

At the same time, in my other blogs, there are other synthetic methods of this type of compound,17570-98-8, 2-(Bromoacetyl)pyridine hydrobromide, and friends who are interested can also refer to it.

Adding a certain compound to certain chemical reactions, such as: 17570-98-8, 2-(Bromoacetyl)pyridine hydrobromide, can increase the reaction rate and produce products with better performance than those obtained under traditional synthetic methods. Here is a downstream synthesis route of the compound, HPLC of Formula: C7H7Br2NO, blongs to pyridine-derivatives compound. HPLC of Formula: C7H7Br2NO

General Procedure 2: Formation of an imidazole by sequential treatment of an amidine with LiHMDS and a heteroaryl-halomethylketone in THF followed by dehydration of the intermediate hvdroxyimidazoli?e in hot acetic acid.; A 1.0 M solution of LiHMDS in THF (Aldrich Chemical Co., 1.0-1.2 equiv, or 2.2 equiv when the heteroaryi-halomethyfketone is a hydrobromide salt) is added dropwise to a solution of the amidine (1.0 equiv) in anhydrous THF (generally 2-4 mL/mmol amidine) at -20 0C to 50C under nitrogen and the resulting solution stirred at about 0 0C for 10-30 min. A solution of the haloketo?e (1.0-1.5 equiv, in equal or greater amount relative to the lithium base) in anhydrous THF (1-3 mL per mmol) is added in one portion. The resulting mixture is stirred in an ice bath for 10-30 min and then at RT for at least 30 min. Water and organic solvent (usually EtOAc or DCM) are added and the product is isolated by extraction into the organic layer which is dried and concentrated. The resulting crude product, which generally contains hydroxy-imidazoline, the target imidazole, and unreacted amidine (HPLCMS analysis) is dissolved in acetic acid (5-25 mUmmol) and heated at 60-1000C for 20-60 min (HPLCMS showing disappearance of the hydroxy-imidazoline peak). This mixture is concentrated, and the crude product isolated by extraction using aqueous NaOH and organic solvent (usually EtOAc or DCM), and residual amidine removed by washing with aqueous citric acid. If not otherwise specified, the product was purified by SGC (gradient of MeOH in DCM, 0.5% NH4OH). In the following Example section, compounds of formula I are designated as Example 1, Example 2, and so on, whereas the corresponding synthetic intermediates are designated Preparation 1 A , Preparation 1 B, or Preparation 2A; Example 4; i-(4-(4-fpvridin-2-vO-1 -fpyrimidin-5-vl)-1 H-imidazol-2-vltohenvl)-1 H-pvrrolof2.3-biDvridine; According to General Procedure 2, NI-(pyrimidi?-5-yl)-4-(1H-pyrrolo[2l3-b]pyridin-1- yl)benzamidine (447 mg, 1.42 mmol) and 2-bromo-1-(pyridin-2-yl)ethanone hydrobromide (400 mg, 1.42 mmol) gave the title substance as a yellow solid. Yield 80 mg, 13.5% of theory. 1H NMR (CDCI3) delta 9.24 (s, 1H), 8.77 (s, 2H)1 8.58 (m, 1H), 8.35 (del, 1H1 J = 1.7, 4.6), 8.13 (d, 1H, J = 7.9), 7.95 (dd, 1H, J =1.5, 7.7), 7.90 (s, 1H), 7.87 (m, 2H), 7.77 (m, 1H), 7.57 (m, 2H), 7.52 (d, 1H, J = 3.7), 7.20 (m, 1H), 7.13 (dd, 1H1 J = 5.0, 7.9), 6.64 (d, 1H, J = 3.7). MS (AP+) m/beta 416 (MH+). IC50 = 13.6 nM

At the same time, in my other blogs, there are other synthetic methods of this type of compound,17570-98-8, 2-(Bromoacetyl)pyridine hydrobromide, and friends who are interested can also refer to it.

Reference:
Patent; PFIZER PRODUCTS INC.; WO2008/4117; (2008); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Some tips on 17570-98-8

Statistics shows that 17570-98-8 is playing an increasingly important role. we look forward to future research findings about 2-(Bromoacetyl)pyridine hydrobromide.

Application of 17570-98-8, With the rapid development and complex challenges of chemical substances, the synthesis of new drugs is usually one of the most effective ways to increase yield.17570-98-8, name is 2-(Bromoacetyl)pyridine hydrobromide, molecular formula is C7H7Br2NO, molecular weight is 280.95, as common compound, the synthetic route is as follows.

EXAMPLE 1a; [(methylethyl)sulfonyl](trans-4-{[(4-(2-pyridyl)(1,3-thiazol-2-yl))amino]methyl}cyclohexyl)amine; N-({[(trans-4-{[(methylethyl)sulfonyl]amino}cyclohexyl)methyl]amino}thioxomethyl)amide (0.60 g, 2.0 mmol) was added to a stirred solution of 2-bromo-1-(2-pyridyl)ethan-1-one hydrobromide (0.57 g, 2.0 mmol) in EtOH (20 mL) at rt followed by the addition of DIEA (1.05 mL, 6.0 mmol). The reaction mixture was heated at reflux for 4 h, cooled to rt, and concentrated in vacuo. The resultant residue was re-dissolved in CHCl3 and washed successively with aqueous citric acid, water and brine. The organic layer was dried over Na2SO4 and concentrated in vacuo. The crude product was purified by silica gel column chromatography (60% EtOAc in Hexanes) to afford the desired product as a tan colored solid (0.56 g, 69%). 1H NMR (CDCl3) delta 8.58 (d, 1H, J=4.8 Hz), 7.89 (dt, 1H, J=7.6 and 1.2 Hz), 7.71 (td, 1H, J=7.8 and 2.0 Hz), 7.17 (td. 1H, J=4.8 and 1.2 Hz), 5.25 (br s, 1H), 3.85 (d, 1H, J=8.4 Hz), 3.25 (br m, 1H), 3.18 (t, 2H, J=6.4 Hz), 2.14 (dt, 2H, J=12.0 and 1.2 Hz), 2.19 (br, d, 2H, J=12.8 Hz), 1.62 (br m, 3H), 1.38 (d, 6H, J=6.8 Hz), 1.25 (dq, 2H, J=12.8 and 1.6 Hz). LC-MS m/e: 395 (M+H)+; tR=2.14 min (Method-A).

Statistics shows that 17570-98-8 is playing an increasingly important role. we look forward to future research findings about 2-(Bromoacetyl)pyridine hydrobromide.

Reference:
Patent; Jubian, Vrej; Packiarajan, Mathivanan; Jimenez, Hermogenes; Reinhard, Emily; US2006/293341; (2006); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Analyzing the synthesis route of 2-(Bromoacetyl)pyridine hydrobromide

Statistics shows that 17570-98-8 is playing an increasingly important role. we look forward to future research findings about 2-(Bromoacetyl)pyridine hydrobromide.

Reference of 17570-98-8, With the rapid development and complex challenges of chemical substances, the synthesis of new drugs is usually one of the most effective ways to increase yield.17570-98-8, name is 2-(Bromoacetyl)pyridine hydrobromide, molecular formula is C7H7Br2NO, molecular weight is 280.95, as common compound, the synthetic route is as follows.

7V,/V-dicyclopropyl-6-ethyl-l-methyl-4-(4-(pyridin-2-yl)thiazol-2-ylamino)-l,6- dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridine-7-carboxamide [00183] A solution of 4-amino-N,N-dicyclopropyl-6-ethyl-l -methyl- 1,6- dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridine-7-carboxamide (example 1J, 70 mg, 0.21 mmol) and benzoyl isothiocyanate (36 mu, 0.27 mmol) in acetone (1 ml) was stirred at room temperature for 1.5h. The solvent was removed in vacuo, the residue was taken up in EtOH (1.5 ml), and K2CO3 (40 mg, 0.290 mmol) was added. The reaction was heated at 60C for 3h. Upon cooling to room temperature, 2-bromo-l- (pyridin-2-yl)ethanone, hydrobromide (139.4 mg, 0.50 mmol) was added and the reaction heated at 80C for 24h. The reaction mixture was cooled to roomtemperature and concentrated. The residue was purified by silica gel chromatography (0-7% MeOH/dichloromethane). Re-purification by preparative HPLC provided 10.2 mg (10% yield) of N,N-dicyclopropyl-6-ethyl-l -methyl -4-(4-(pyridin-2-yl)thiazol-2- ylamino)-l,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridine-7-carboxamide as a brown solid.[00184] MS (ESI) rt = 1.78 min, m/z 499 (M+H).[00185] 1H MR (DMSO-d6) delta ppm 10.9 (s, 1 H), 8.2 (bs, 1 H), 7.81 (d, 1 H), 7.75 (s, 1H), 3.92 (m, 4H), 3.77 (q, 2H, J= 7.8 Hz), 2.52-2.81 (m, 7H).

Statistics shows that 17570-98-8 is playing an increasingly important role. we look forward to future research findings about 2-(Bromoacetyl)pyridine hydrobromide.

Reference:
Patent; BRISTOL-MYERS SQUIBB COMPANY; PURANDARE, Ashok V.; GREBINSKI, James W.; HART, Amy; INGHRIM, Jennifer; SCHROEDER, Gretchen; WAN, Honghe; WO2011/28864; (2011); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Extended knowledge of 17570-98-8

With the rapid development of chemical substances, we look forward to future research findings about 17570-98-8.

The major producers of chemicals have been the Europe, Japan and China. Due to the growing call for a cleaner, greener environment, people will have to find innovative ways to maintain their relevance. Here is a compound 17570-98-8, name is 2-(Bromoacetyl)pyridine hydrobromide. This compound has unique chemical properties. The synthetic route is as follows. SDS of cas: 17570-98-8

NaH (60%) (120 mg, 3 mmol) was added into a solution of dichloro-2- (2,2,2-trifluoro-ethyl)-1 H-benzoimidazole (269 mg, 1 mmol) in DMF (5 ml) at O0C. The resulting mixture was stirred at 0C for half hour. 2-bromo-1 -(2- pyridiny)-l-ethanone hydrobromide (421.4 mg, 1.5 mmol) was then added to the reaction mixture at 0C. The reaction temperature was raised to 25C and then the reaction mixture was stirred for 18 hours. NH4CI (aq.) was added and extracted with EtOAc. The organic layer was washed with brine, then dried over anhydrous MgSO^ The solvent was distilled out under reduced pressure. Column chromatography (silica gel, EtOAc / hexanes 0% to 70%) yielded the title compound as a yellow solid.MS m/z (M+H) 388, (M-H) 386.

With the rapid development of chemical substances, we look forward to future research findings about 17570-98-8.

Reference:
Patent; JANSSEN PHARMACEUTICA N.V.; WO2006/39215; (2006); A2;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

A new synthetic route of 17570-98-8

The synthetic route of 17570-98-8 has been constantly updated, and we look forward to future research findings.

Application of 17570-98-8 , The common heterocyclic compound, 17570-98-8, name is 2-(Bromoacetyl)pyridine hydrobromide, molecular formula is C7H7Br2NO, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc., below Introduce a new synthetic route.

N-({[(fra/?s-4-{[(methylethyl)sulfonyl]amino}cyclohexyl)methyl]amino}thioxomethyl) amide (0.60 g, 2.0 mmol) was added to a stirred solution of 2-bromo-1-(2- pyridyl)ethan-1-one hydrobromide (0.57 g, 2.0 mmol) in EtOH (20 ml_) at rt followed by the addition of DIEA (1.05 ml_, 6.0 mmol). The reaction mixture was heated at reflux for 4 h, cooled to rt, and concentrated in vacuo. The resultant residue was re- dissolved in CHCI3 and washed successively with aqueous citric acid, water and brine. The organic layer was dried over Na2SO4 and concentrated in vacuo. The crude product was purified by silica gel column chromatography (60 % EtOAc in Hexanes) to afford the desired product as a tan colored solid (0.56 g, 69 %). 1H NMR (CDCI3) delta 8.58 (d, 1 H, J=4.8 Hz), 7.89 (dt, 1 H, J=7.6 and 1.2 Hz), 7.71 (td, 1 H, J=7.8 and 2.0 Hz), 7.17 (td. 1 H, J=4.8 and 1.2Hz), 5.25 (br s, 1 H), 3.85 (d, 1 H1 J=8.4 Hz), 3.25 (br m, 1 H), 3.18 (t, 2H, J=6.4 Hz), 2.14 (dt, 2H, J=12.0 and 1.2 Hz), 2.19 (br, d, EPO 2H, J=12.8 Hz), 1.62 (br m, 3H), 1.38 (d, 6H, J=6.8 Hz), 1.25 (dq, 2H, J=12.8 and 1.6 Hz). LC-MS m/e: 395 (M+H)+; tR = 2.14 min (Method-A).

The synthetic route of 17570-98-8 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; H. LUNDBECK A/S; WO2007/2126; (2007); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

A new synthetic route of 17570-98-8

The synthetic route of 17570-98-8 has been constantly updated, and we look forward to future research findings.

Application of 17570-98-8 , The common heterocyclic compound, 17570-98-8, name is 2-(Bromoacetyl)pyridine hydrobromide, molecular formula is C7H7Br2NO, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc., below Introduce a new synthetic route.

N-({[(fra/?s-4-{[(methylethyl)sulfonyl]amino}cyclohexyl)methyl]amino}thioxomethyl) amide (0.60 g, 2.0 mmol) was added to a stirred solution of 2-bromo-1-(2- pyridyl)ethan-1-one hydrobromide (0.57 g, 2.0 mmol) in EtOH (20 ml_) at rt followed by the addition of DIEA (1.05 ml_, 6.0 mmol). The reaction mixture was heated at reflux for 4 h, cooled to rt, and concentrated in vacuo. The resultant residue was re- dissolved in CHCI3 and washed successively with aqueous citric acid, water and brine. The organic layer was dried over Na2SO4 and concentrated in vacuo. The crude product was purified by silica gel column chromatography (60 % EtOAc in Hexanes) to afford the desired product as a tan colored solid (0.56 g, 69 %). 1H NMR (CDCI3) delta 8.58 (d, 1 H, J=4.8 Hz), 7.89 (dt, 1 H, J=7.6 and 1.2 Hz), 7.71 (td, 1 H, J=7.8 and 2.0 Hz), 7.17 (td. 1 H, J=4.8 and 1.2Hz), 5.25 (br s, 1 H), 3.85 (d, 1 H1 J=8.4 Hz), 3.25 (br m, 1 H), 3.18 (t, 2H, J=6.4 Hz), 2.14 (dt, 2H, J=12.0 and 1.2 Hz), 2.19 (br, d, EPO 2H, J=12.8 Hz), 1.62 (br m, 3H), 1.38 (d, 6H, J=6.8 Hz), 1.25 (dq, 2H, J=12.8 and 1.6 Hz). LC-MS m/e: 395 (M+H)+; tR = 2.14 min (Method-A).

The synthetic route of 17570-98-8 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; H. LUNDBECK A/S; WO2007/2126; (2007); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem