Improved Synthesis of 2‐Chloro‐3‐amino‐4‐methylpyridine
Qian Zhao, Hangeng Chen, Chao Qian, Xinzhi Chen
Abstract
Qian Zhao, Hangeng Chen, Chao Qian, Xinzhi Chen
Abstract
2‐Chloro‐3‐amino‐4‐methylpyridine (1), a key intermediate in the synthesis of nervirapine, was prepared from 2‐cyanoacetamide and 4,4‐dimethoxyl‐2‐butanone via condensation, cyclization, one‐pot reaction of chlorination and hydrolysis, and Hofmann reaction. Utilization of the quadratic orthogonal test resulted in a high yield (62.1%) of the whole process.
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2‐Chloro‐3‐amino‐4‐methylpyridine (1), a key intermediate in the synthesis of nervirapine, was prepared from 2‐cyanoacetamide and 4,4‐dimethoxyl‐2‐butanone via condensation, cyclization, one‐pot reaction of chlorination and hydrolysis, and Hofmann reaction. Utilization of the quadratic orthogonal test resulted in a high yield (62.1%) of the whole process.
Key concepts: Chemistry, Yield (engineering), Cyanoacetamide, Condensation, Hydrolysis, Organic chemistry, Medicinal chemistry, Combinatorial chemistry