Electric Literature of 1990-90-5, 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.1990-90-5, name is 3-Methylpyridin-4-amine, molecular formula is C6H8N2, molecular weight is 108.14, as common compound, the synthetic route is as follows.
To a solution of 3-methylpyridin-4-amine (10 g, 92.6 mmol) in THF (100 ml.) was added TEA (14 g, 138 mmol) and DMAP (1 .12 g, 9.25 mmol) followed by addition of (Boc)20 (22.2 g, 101 mmol) at 0 C. The reaction mixture was stirred at rt for 16h. Progress of the reaction was monitored by TLC and LCMS. After completion, the reaction mixture was concentrated under vacuum. The residue was diluted with water (50 ml.) and extracted with DCM (3 x 70 ml_). The organic layer was separated, dried over anhydrous Na2S04 and concentrated under vacuum to afford 16.2 g of tert-butyl A/-(3-methylpyridin-4-yl)carbamate a49, which was used in next step without further purification. LCMS (ES+): 209 (M+H)+, 96% purity. 1H NMR (400 MHz, DMSO-cfe) delta 8.76 (s, 1 H), 8.22-8.26 (m, 2H), 7.62-7.66 (m, 1 H), 2.18 (s, 3H), 1 .48 (s, 9H).
The chemical industry reduces the impact on the environment during synthesis 1990-90-5, I believe this compound will play a more active role in future production and life.
Reference:
Patent; UCB BIOPHARMA SPRL; ATES, Ali; JNOFF, Eric; PROVINS, Laurent; VALADE, Anne; HALL, Adrian; (97 pag.)WO2017/178377; (2017); A1;,
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