Category: 56622-54-9

Gunzner-Toste, Janet; Zhao, Guiling; Bauer, Paul; Baumeister, Timm; Buckmelter, Alexandre J.; Caligiuri, Maureen; Clodfelter, Karl H.; Fu, Bang; Han, Bingsong; Ho, Yen-Ching; Kley, Nikolai; Liang, Xiaorong; Liederer, Bianca M.; Lin, Jian; Mukadam, Sophie; O’Brien, Thomas; Oh, Angela; Reynolds, Dominic J.; Sharma, Geeta; Skelton, Nicholas; Smith, Chase C.; Sodhi, Jasleen; Wang, Weiru; Wang, Zhongguo; Xiao, Yang; Yuen, Po-wai; Zak, Mark; Zhang, Lei; Zheng, Xiaozhang; Bair, Kenneth W.; Dragovich, Peter S. published the artcile< Discovery of potent and efficacious urea-containing nicotinamide phosphoribosyltransferase (NAMPT) inhibitors with reduced CYP2C9 inhibition properties>, Reference of 56622-54-9, the main research area is urea containing nicotinamide phosphoribosyltransferase inhibitor reduced CYP2C9 inhibition preparation; pharmacokinetic antitumor activity urea containing benzenesulfonamide.

Potent, reversible inhibition of the cytochrome P 450 CYP2C9 isoform was observed in a series of urea-containing nicotinamide phosphoribosyltransferase (NAMPT) inhibitors. This unwanted property was successfully removed from the described inhibitors through a combination of structure-based design and medicinal chem. activities. An optimized compound, I, which did not inhibit CYP2C9 exhibited potent anti-NAMPT activity (BC NAMPT IC50 = 3 nM; A2780 antiproliferative IC50 = 70 nM), good mouse PK properties, and was efficacious in an A2780 mouse xenograft model. The crystal structure of this compound in complex with the NAMPT protein is also described.

Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 56622-54-9 belongs to class pyridine-derivatives, and the molecular formula is C7H10N2, Reference of 56622-54-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Shipe, William D.; Sharik, Steven S.; Barrow, James C.; McGaughey, Georgia B.; Theberge, Cory R.; Uslaner, Jason M.; Yan, Youwei; Renger, John J.; Smith, Sean M.; Coleman, Paul J.; Cox, Christopher D. published the artcile< Discovery and Optimization of a Series of Pyrimidine-Based Phosphodiesterase 10A (PDE10A) Inhibitors through Fragment Screening, Structure-Based Design, and Parallel Synthesis>, Application In Synthesis of 56622-54-9, the main research area is pyrimidine derivative PDE10A inhibitor screening discovery preparation structure.

Screening of a fragment library for PDE10A inhibitors identified a low mol. weight pyrimidine hit with PDE10A Ki of 8700 nM and LE of 0.59. Initial optimization by catalog followed by iterative parallel synthesis guided by X-ray cocrystal structures resulted in rapid potency improvements with minimal loss of ligand efficiency. Compound 15h, with PDE10A Ki of 8.2 pM, LE of 0.49, and >5000-fold selectivity over other PDEs, fully attenuates MK-801-induced hyperlocomotor activity after i.p. dosing.

Journal of Medicinal Chemistry published new progress about Antipsychotics. 56622-54-9 belongs to class pyridine-derivatives, and the molecular formula is C7H10N2, Application In Synthesis of 56622-54-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Heath, Julie A.; Mehrotra, Mukund M.; Chi, Shannon; Yu, Jin-Chen; Hutchaleelaha, Athiwat; Hollenbach, Stanley J.; Giese, Neill A.; Scarborough, Robert M.; Pandey, Anjali published the artcile< Identification of 4-piperazin-1-yl-quinazoline template based aryl and benzyl thioureas as potent, selective, and orally bioavailable inhibitors of platelet-derived growth factor (PDGF) receptor>, SDS of cas: 56622-54-9, the main research area is PDGF receptor inhibitor thiourea derivative structure activity cancer.

4-[4-(N-Substituted-thio-carbamoyl)-1-piperazinyl]-6-methoxy-7-alkoxyamino-quinazoline derivatives such as 14 (CT53986) have been identified to be potent and selective inhibitors of the phosphorylation of PDGFR. SAR-investigations are described in the arylamine segment, C-7 appendage, and the thiourea moiety. Bioisosteres of thiourea (cyanoguanidine), and of quinazoline (quinoline-3-carbonitrile) were synthesized and are compared for their in vitro inhibitory activity. PK profiles of the optimized compounds in rat, dog, and cynomolgus monkey are described.

Bioorganic & Medicinal Chemistry Letters published new progress about c-Kit proteins Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 56622-54-9 belongs to class pyridine-derivatives, and the molecular formula is C7H10N2, SDS of cas: 56622-54-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Zhang, Wenming; Holyoke, Caleb W. Jr.; Pahutski, Thomas F.; Lahm, George P.; Barry, James D.; Cordova, Daniel; Leighty, Robert M.; Singh, Vineet; Vicent, Daniel R.; Tong, My-Hanh T.; Hughes, Kenneth A.; McCann, Stephen F.; Henry, Yewande T.; Xu, Ming; Briddell, Twyla A. published the artcile< Mesoionic pyrido[1,2-a]pyrimidinones: Discovery of triflumezopyrim as a potent hopper insecticide1>, Synthetic Route of 56622-54-9, the main research area is mesoionic pyrido pyrimidinone preparation hopper insecticidal activity SAR; triflumezopyrim preparation hopper insecticidal activity SAR; Acetylcholine receptor; Inhibitor; Insecticide; Mesoionic; Pyrido[1,2-a]pyrimidinone; Triflumezopyrim.

A novel class of mesoionic pyrido[1,2-a]pyrimidinones has been discovered with exceptional insecticidal activity controlling a number of insect species. In this communication, we report the part of the optimization program which led to the discovery of triflumezopyrim (I) as a highly potent insecticide controlling various hopper species. Our efforts in discovery, synthesis, structure-activity relationship elucidation, and biol. activity evaluation are also presented.

Bioorganic & Medicinal Chemistry Letters published new progress about Acute toxicity. 56622-54-9 belongs to class pyridine-derivatives, and the molecular formula is C7H10N2, Synthetic Route of 56622-54-9.

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Synthetic Route of 56622-54-9, 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.56622-54-9, name is (6-Methylpyridin-3-yl)methanamine, molecular formula is C7H10N2, molecular weight is 122.17, as common compound, the synthetic route is as follows.

2-Fluoro-N-((6-methylpyridin-3-yl)methyl)-9H-purin-6-amineTo a stirred solution of 6-chloro-2-fluoropurine ( 0.4g, 2.3 mmol) in n-BuOH (50 ml) under an argon atmosphere at O0C, was added DIEA (2.5 ml, 14.7 mmol) followed by (6-methylpyridin-3-yl)methanamine (0.36g, 2.95 mmol). The reaction mixture was stirred at this temperature for 1 h and then allowed to return to room temperature and stirred for 4h, it was still seen incomplete, hence heated the reaction to 1000C and left at that temperature for 8h. The solvent was evaporated in vacuo and the residue was purified by gradient column chromatography on silica gel, eluted with CHCl3 :MeOH (100:0 ? 90:10), to afford the product as a white solid; Yield: 0.38 g (65%) deltaH CDCl3, 250 MHz) 2.44 ( 3 H, s, CH3), 3.66 – 3.57 ( 2 H, m, NHCH2), 4.63 ( 1 H, s, br, NH),7.25 ( 1 H, d, J 7.5, ArH), 7.71 (1 H, dd, J 2.5, 7.5, ArH), 8.14 ( 1 H, s, ArH), 8.49 (1 H, s, ArH), 9.07 (1 H, s, br, NH); deltac ( CDCl3, 250 MHz) 159.12 (C), 158.62 (C), 157.61 (C), 155.56 (C), 147.44 (CH), 146.99 (CH), 136.32 (C), 123.05 (2 x CH), 119.42 (C), 41.64 (CH2), 18.47 (CH3); m/z 259.2 (M + H)

Statistics shows that 56622-54-9 is playing an increasingly important role. we look forward to future research findings about (6-Methylpyridin-3-yl)methanamine.

Reference:
Patent; CYCLACEL LIMITED; CANCER RESEARCH TECHNOLOGY LIMITED; WO2008/122767; (2008); A2;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Reference of 56622-54-9, Researchers who often do experiments know that organic synthesis is a process of preparing more complex target molecules from simple raw materials through one or more chemical reactions. Generally, it requires fewer steps,and cheap raw materials. 56622-54-9, name is (6-Methylpyridin-3-yl)methanamine. A new synthetic method of this compound is introduced below.

Into a round-bottom flask were charged 3-(5-methylpyridin-2-yl)-5-(pyrrolidine-l – carbonyl)benzoic acid (80 mg, 0.26 mmol), (6-methylpyridin-3-yl)methanamine (60 mg, 0.49 mmol), N- (3-dimethylaminopropyl)-N’-ethylcarbodiimide hydrochloride (90 mg, 0.47 mmol), 1- hydroxybenzotriazole hydrate (80 mg, 0.52 mmol), NN-diisopropylethylamine (80 mg, 0.62 mmol) and methylene chloride (5 mL). The mixture was stirred at room temperature overnight and then concentrated. The residue was purified via preparative HPLC to afford the desired product as a white solid.LC-MS: 415.5 [M+l]+; 1H NMR (400 MHz, CD3OD): 8.56 (t, J = 1.7 Hz, IH), 8.53-8.52 (m, IH), 8.46 (d, J = 2.1 Hz, IH), 8.29 (t, J = 1.6 Hz, IH), 8.04 (t, J = 1.6 Hz, IH), 7.89 (d, J = 8.1 Hz, IH), 7.81-7.77 (m, 2H), 7.32 (d, J = 8.0 Hz, IH), 4.63 (s, 2H), 3.66 (t, J = 7.0 Hz, 2H), 3.54 (t, J = 6.7 Hz, 2H), 2.54 (s, 3H),2.43 (s, 3H), 2.05-1.94 (m, 4H).

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,56622-54-9, its application will become more common.

Reference:
Patent; RENOVIS, INC.; WO2009/110985; (2009); A2;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Application of 56622-54-9, 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.56622-54-9, name is (6-Methylpyridin-3-yl)methanamine, molecular formula is C7H10N2, molecular weight is 122.17, as common compound, the synthetic route is as follows.

[0557] To a solution of compound VII (0.5 g, 1.39 mmol, 1 eq) in DMF (50 mL) were added HATU (0.7 g, 1.8 mmol, 1.3 eq) and DIPEA (0.74 mL, 4.17 mmol, 3 eq) under argon atmosphere at 0 C. A DMF solution of C-(6-methyl-pyridin-3-yl)-methylamine (0.25 g, 2.09 mmol, 1.5 eq) was added and the resulting mixture was stirred at 23 C for 16 h. The mixture was diluted with ice water (40 mL) and the organic components were extracted with EtOAc (2 x 50 mL) and 10% MeOH/CH2C12 (50 mL), and the combined extracts were washed with brine (50 mL). The organic layer was dried over anhydrous sodium sulfate, filtered and concentrated under reduced pressure to provide the crude compound. The crude product was purified by flash Combiflash chromatography using 100-200 mesh silica gel eluting with 5% MeOH/CH2C12 to obtain compound (0.4 g, 62%) as an orange solid. 1H NMR (400 MHz, DMSO-d6) oe 9.53 (t, 1H, J = 6 Hz), 9.18 (s, 1H), 8.47 (s, 1H), 8.37 (s, 1H), 7.94 (s, 1H),7.70-7.44 (m, 2H), 7.23 (d, 1H, J = 8 Hz), 4.53 (d, 2H, J = 5 Hz), 2.45 (s, 3H). LCMS: m/z =463.0 [M+j, 465.0 [M+21, RT = 1.94 minutes; (Program Ri, Column W).

Statistics shows that 56622-54-9 is playing an increasingly important role. we look forward to future research findings about (6-Methylpyridin-3-yl)methanamine.

Reference:
Patent; ASANA BIOSCIENCES, LLC; THOMPSON, Scott; VENKATESAN, Aranapakam; PRIESTLEY, Tony; KUNDU, Mrinal; SAHA, Ashis; WO2015/95128; (2015); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Synthetic Route of 56622-54-9, 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. 56622-54-9, name is (6-Methylpyridin-3-yl)methanamine, molecular formula is C7H10N2, 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.

To a mixture of 5-(ethoxycarbonyl)-4′-methylbiphenyl-3-carboxylic acid (1.5 g, 5.3 mmol), N-(3-dimethylaminopropyl)-N’-ethylcarbodiimide hydrochloride (2.0 g, 10 mmol), 1- hydroxybenzotriazole hydrate (0.32 g, 2.1 mmol), and CH2Cl2 (50 mL) were added (6-methylpyridin-3- yl)methanamine (0.97 g, 7.9 mmol) and NN-diisopropylethylamine (1.8 mL, 10 mmol). The mixture was stirred at room temperature for 4h, and then washed with water and aq. Na2CO3 solution, dried (Na2SO4), and concentrated in vacuo. The residue was purified by silica gel column to afford a white foam. LC-MS: 389.4 [M+l]+; 1H NMR (400 MHz, CDCl3): 8.53 (d, IH, J = 2.0 Hz), 8.39 (t, IH, J = 1.6 Hz), 8.29 (t, IH, J = 1.6 Hz), 8.26 (t, IH, J = 1.6 Hz), 7.66 (dd, IH, J = 8.0, 2.0 Hz), 7.55 (d, 2H, J = 8.4 Hz), 7.28 (d, 2H, J = 8.0 Hz), 7.17 (d, IH, J = 8.0 Hz), 6.64 (m, IH), 4.67 (d, 2H, J = 5.6 Hz), 4.42 (q, 2H, J = 7.2 Hz), 2.57 (s, 3H), 2.41 (s, 3H), 1.42 (t, 3H, J = 7.2 Hz).

According to the analysis of related databases, 56622-54-9, the application of this compound in the production field has become more and more popular.

Reference:
Patent; RENOVIS, INC.; WO2009/110985; (2009); A2;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

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. 56622-54-9, name is (6-Methylpyridin-3-yl)methanamine, molecular formula is C7H10N2, 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. Safety of (6-Methylpyridin-3-yl)methanamine

[0340] To a stirred solution of compound XI (0.15 g, 0.42 mmol, leq) in CH2C12: DMF (1:5, 20 mL) were added DIPEA (0.22 mL, 1.2 mmol, 3 eq) and HATU (0.2 g, 0.54 mmol, 1.3 eq) and the resulting mixture was stirred at 0 C for 15 mm. To the mixture was added C-(6-methyl-pyridin-3-yl)-methylamine (0.13 g, 0.85 mmol, 2 eq) and the resulting mixture allowed to stir at 23 C for another 16 h. From the mixture, solvent was removed in vacuo, the residue was diluted with EtOAc and washed with saturated aqueous sodium bicarbonate solution, aqueous ammonium chloride solution and brine. The organic layer was dried over anhydrous sodium sulfate, filtered and concentrated to dryness. The crude product was purified by silica gel (230-400 mesh) column chromatography eluting with 0-10% methanol/CH2C12 to obtain the title compound (30 mg, 16%) as an off white solid. 1H NMR (DMSO-d6) oe 9.37 (t, 1H, J = 6 Hz), 9.10 (d, 1H, J = 1 Hz), 8.42 (d, 1H, J = 2 Hz), 7.90 (d, 1H, J = 1 Hz), 7.84 (s, 1H), 7.68 (d, 1H, J = 1 Hz), 7.63 (dd, 1H, J = 2, 8 Hz), 7.43 (d, 1H, J= 4 Hz), 7.22 (d, 1H, J = 8 Hz), 7.03 (d, 1H, J = 3 Hz), 6.35 (s, 1H), 4.48 (d, 2H, J = 6 Hz),2.62 (q, 2H, J= 8Hz), 2.55 (s, 3H), 2.50 (s, 3H), 1.11 (t, 3H, J= 8Hz). LCMS: mlz = 457.0[M+Hj , RT = 3.21 minutes, (Program P1, Column Y).

With the rapid development of chemical substances, we look forward to future research findings about 56622-54-9.

Reference:
Patent; ASANA BIOSCIENCES, LLC; THOMPSON, Scott; VENKATESAN, Aranapakam; PRIESTLEY, Tony; KUNDU, Mrinal; SAHA, Ashis; WO2015/95128; (2015); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

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.56622-54-9, name is (6-Methylpyridin-3-yl)methanamine, molecular formula is C7H10N2, molecular weight is 122.17, as common compound, the synthetic route is as follows.Quality Control of (6-Methylpyridin-3-yl)methanamine

Into a round bottom flask were combined 5-formyl-4′-methylbiphenyl-3-carboxylic acid(3.00 g, 12.5 mmol), (6-methylpyridin-3-yl)methanamine (1.91 g, 15.6 mmol), NN-diisopropylethylamine (6.46 g, 49.9 mmol) and NN-dimethylformamide (97 mL). NN,N’,N’-Tetramethyl-O-(7-azabenzotriazol- l-yl)uronium hexafluorophosphate (9.50 g, 25.0 mmol) was added in one portion and the mixture was heated at 60 0C for 2 h. After cooling, the mixture was poured onto saturated sodium bicarbonate (200 mL) and extracted with ethyl acetate (3 x 100 mL). The combined extracts were dried over sodium sulfate and concentrated in vacuo. The residue was purified by column chromatography using methylene chloride:methanol gradient (0-10%) to afford the title compound. LC-MS: 346.2 [M+l ]+; 1H NMR (400 MHz, DMSO-d6): 10.14 (s, IH), 8.46-8.43 (m, 2H), 8.37-8.33 (m, 2H), 7.72 (d, 2H, J = 8.0 Hz), 7.64 (dd, IH, J = 8.0 Hz), 7.34 (d, 2H, J = 7.9 Hz), 7.22 (d, 2H, J = 7.9 Hz), 4.51 (d, 2H, J = 5.9 Hz), 2.44 (s, 3H), 2.37 (s, 3H).

At the same time, in my other blogs, there are other synthetic methods of this type of compound,56622-54-9, (6-Methylpyridin-3-yl)methanamine, and friends who are interested can also refer to it.

Reference:
Patent; RENOVIS, INC.; WO2009/110985; (2009); A2;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem