爱维莫潘的合成
发布时间：2018-10-29 21:45
【摘要】：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)。
[Abstract]:Michael addition reaction of 3- [(3RH4R) -3O4-Dimethylpiperidine-4-yl] phenol (2) with ethyl 2-benzylacrylate, and then crystallization of hydrogen chloride to obtain (S) -2-benzyl-3- [(3R, 3R, 3R)] 4R) -4- (3-hydroxyphenyl) -3- (4-dimethylpiperidine-1-yl) ethyl propionate hydrochloride (3), the mother liquor of crystallization was applied by racemization cycle, the yield of 3 was 60.3 in turn hydrolyzed, the glycine isobutyl ester was condensed, Avermosin was prepared by hydrolysis with a total yield of about 45% (in 2).
【作者单位】： 中国医药工业研究总院上海医药工业研究院创新药物与制药工艺国家重点实验室;
【分类号】：R914.5
本文编号：2298919
[Abstract]:Michael addition reaction of 3- [(3RH4R) -3O4-Dimethylpiperidine-4-yl] phenol (2) with ethyl 2-benzylacrylate, and then crystallization of hydrogen chloride to obtain (S) -2-benzyl-3- [(3R, 3R, 3R)] 4R) -4- (3-hydroxyphenyl) -3- (4-dimethylpiperidine-1-yl) ethyl propionate hydrochloride (3), the mother liquor of crystallization was applied by racemization cycle, the yield of 3 was 60.3 in turn hydrolyzed, the glycine isobutyl ester was condensed, Avermosin was prepared by hydrolysis with a total yield of about 45% (in 2).
【作者单位】： 中国医药工业研究总院上海医药工业研究院创新药物与制药工艺国家重点实验室;
【分类号】：R914.5
【共引文献】
相关硕士学位论文 前1条
1 侯清;通腑汤治疗腹部术后早期肠麻痹的临床研究[D];北京中医药大学;2012年
，本文编号：2298919
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