【摘要】：3-[(3R,4R)-3,4-二甲基哌啶-4-基]苯酚(2)與2-芐基丙烯酸乙酯發(fā)生Michael加成反應(yīng),然后通氯化氫氣體析晶得(S)-2-芐基-3-[(3R,4R)-4-(3-羥基苯基)-3,4-二甲基哌啶-1-基]丙酸乙酯鹽酸鹽(3),析晶母液經(jīng)消旋化循環(huán)套用,3的收率為60%。3依次經(jīng)水解、甘氨酸異丁酯縮合、水解制得愛維莫潘,總收率約45%(以2計)。
[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).
【作者單位】： 中國醫(yī)藥工業(yè)研究總院上海醫(yī)藥工業(yè)研究院創(chuàng)新藥物與制藥工藝國家重點實驗室;
【分類號】：R914.5

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1 侯清;通腑湯治療腹部術(shù)后早期腸麻痹的臨床研究[D];北京中醫(yī)藥大學(xué);2012年

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