Category: 1403257-80-6

Application of 1403257-80-6, 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. 1403257-80-6, name is 5-Bromo-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-2-methylbenzamide, molecular formula is C23H30BrN3O3, 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.

Step 1: Synthesis of N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-5-(6-formylpyridin-3-yl)-2-methylbenzamide To a stirred solution of 5-bromo-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-2-methylbenzamide (1 g, 2.15 mmol) and (6-formylpyridin-3-yl)boronic acid (0.539 g, 2.31 mmol) in dioxane/water mixture (15 mL+3 mL), Na2CO3 (0.82 g, 7.74 mmol) was added and solution purged with argon for 15 min. Then Pd (PPh3)4 (0.288 g, 0.25 mmol) was added and argon was purged again for 10 min. Reaction mass was heated at 80 C. for 2 h. On completion, reaction mixture was diluted with water and extracted with 10% MeOH/DCM. Combined organic layers were dried over Na2SO4 and solvent removed under reduced pressure to afford crude material which was purified by column chromatography over silica gel to afford the desired compound (0.60 g, 57%).

While traditionally a conservative industry, chemical producers will need to modernize their PR strategies to stay relevant.we look forward to future research findings about 1403257-80-6, 5-Bromo-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-2-methylbenzamide.

Reference:
Patent; KUNTZ, KEVIN W.; CHESWORTH, RICHARD; DUNCAN, KENNETH W.; KEILHACK, HEIKE; WARHOLIC, NATALIE; KLAUS, CHRISTINE; ZHENG, WANJUN; SEKI, MASASHI; SHIROTORI, SYUJI; KAWANO, SATOSHI; US2012/264734; (2012); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Adding a certain compound to certain chemical reactions, such as: 1403257-80-6, 5-Bromo-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-2-methylbenzamide, 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, COA of Formula: C23H30BrN3O3, blongs to pyridine-derivatives compound. COA of Formula: C23H30BrN3O3

11115] To a solution of methyl 3-methyl-2-(3-(6-(4-(4,4, 5,5-tetramethyl-1 ,3,2-dioxaborolan-2-yl)phenoxy)hexy- loxy)isoxazol-5-yl)butanoate (200 mg, 0.41 mmol) and 5-bromo-N-((4,6-dimethyl-2-oxo-1 ,2-dihydropyridin-3-yl) methyl)-3-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-2-meth- ylbenzamide (220 mg, 0.45 mmol) in dioxane (5 mE) and H20 (0.5 mE) was added cesium carbonate (450 mg, 1.38 mmol), Tri-tert-butylphosphine tetrafluoroborate (40 mg, 0.14 mmol), [1,1 ?-l3is(diphenylphosphino)ferrocene]dichlo- ropalladium(II) (46 mg, 0.06 mmol), stirred at 100 C. for 2 hours under nitrogen. The mixture was quenched with water (10 mE) and extracted with dichloromethane methanol (10:1) (10 mEx3), and the combined organic layer was washed with brine (5 mEx2), dried over anhydrous sodium sulfate, filtered and concentrated in vacuo and purified by pre-TEC (dichloromethanemethanol=1 5:1) to give methyl 2-(3-(5-(3?-((4,6-dimethyl-2-oxo-1 ,2-dihydropyridin-3-yl)methylcarbamoyl)-5?-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4?-methylbiphenyl-4-yloxy)pentyloxy)isoxazol-5-yl)-3-methylbutanoate (110 mg, 36% yield) as a yellow solid. ECMS (Agilent ECMS 1200-6 120, Column:Waters X-l3ridge C18 (50 mmx4.6 mmx3.5 pm); Column Temperature: 40 C.; Flow Rate: 2.0 mE/mm; Mobile Phase:from 90% [(total 10mM AcONH4) water/CH3CN=900/100 (v/v)] and 10% [(total 10 mM AcONH4) water CH3CN=100/900 (vv)] to 10% [(total 10 mM AcONH4) water/CH3CN=900/100 (v/v)] and 90% [(total 10 mM AcONH4) water/CH3CN=100/900 (v/v)] in 1.6 mm, then under this condition for 2.4 mm, finally changed to 90% [(total 10 mM AcONH4) water/CH3CN=900/100 (v/v)] and 10% [(total 10mM AcONH4) water/CH3CN=1 00/900 (v/v)] in 0.1 mm and under this condition for 0.7 mm). Purity is 76.61%, Rt=1.275 mm.; MS Calcd.: 756.93; MS Found:757.3 [M+H].

The synthetic route of 1403257-80-6 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Arvinas, Inc.; Crew, Andrew P.; Snyder, Lawrence B.; Wang, Jing; Dong, Hanqing; Qian, Yimin; Berlin, Michael; (513 pag.)US2018/177750; (2018); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem