New downstream synthetic route of 4-Amino-2-picoline

The synthetic route of 18437-58-6 has been constantly updated, and we look forward to future research findings.

Related Products of 18437-58-6 , The common heterocyclic compound, 18437-58-6, name is 4-Amino-2-picoline, molecular formula is C6H8N2, 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.

1003651 Step A: 2-Methylpyridin-4-amine (0.28 g, 2.6 mmol) was placed in THF (5 mL) and cooled to -78C. t-BuLi (1.5 mE, 2.6 mmol) was added dropwise, and the solution was warmed to 0C for 30 minutes. This solution was then added dropwise to a -78C THF solution (5 mL) of (5)-i -(2-(tert-butyldimethylsilyloxy)- 1 -(4-chloro-3 -fluorophenyl)ethyl)-4-(2-(methylsulfonyl)pyrimidin-4-yl)pyridin-2( 1 11)-one (0.070 g, 0.13 mmol). The reaction was stirred for an additional 30 minutes at -78C, then poured into water, and extracted with DCM. The combined organic fractions were dried (MgSO4), filtered, and concentrated to give the crude product, which was purified by column chromatography (500:10-500:20 DCM/MeOH) to give the product (5)-i -(2-(tert-butyldimethylsilyloxy)- 1 -(4-chloro-3 – fluorophenyl)ethyl)-4-(2-((2-methylpyridin-4-yl)amino)pyrimidin-4-yl)pyridin-2( 111)-one(0.028 g, 38% yield).

The synthetic route of 18437-58-6 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; ARRAY BIOPHARMA INC.; GENENTECH, INC.; BLAKE, James F.; CHICARELLI, Mark Joseph; GARREY, Rustam Ferdinand; GAUDINO, John; GRINA, Jonas; MORENO, David A.; MOHR, Peter J.; REN, Li; SCHWARZ, Jacob; CHEN, Huifen; ROBARGE, Kirk; ZHOU, Aihe; WO2013/130976; (2013); A1;,
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem