论文部分内容阅读
3-[(3R,4R)-3,4-二甲基哌啶-4-基]苯酚(2)与2-苄基丙烯酸乙酯发生Michael加成反应,然后通氯化氢气体析晶得(S)-2-苄基-3-[(3R,4R)-4-(3-羟基苯基)-3,4-二甲基哌啶-1-基]丙酸乙酯盐酸盐(3),析晶母液经消旋化循环套用,3的收率为60%。3依次经水解、甘氨酸异丁酯缩合、水解制得爱维莫潘,总收率约45%(以2计)。
The Michael addition reaction of 3 - [(3R, 4R) -3,4-dimethylpiperidin-4-yl] phenol and ethyl 2-benzyl acrylate followed by crystallization from hydrogen chloride gas gave ) Ethyl 3-r (3R, 4R) -4- (3-hydroxyphenyl) -3,4-dimethylpiperidin- 1 -yl] propionate hydrochloride (3) , The crystallization of the mother liquid by the race cycle application, 3 yield of 60%. 3 followed by hydrolysis, glycine isobutyl condensation, hydrolysis obtained avermectin, the total yield of about 45% (2 dollars).