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化学学报
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化学学报 ›› 2001, Vol. 59 ›› Issue (8): 1317-1322. 上一篇    下一篇

研究论文

含(1-芳乙酰胺基-2-叔胺基)乙烷结构的六氢-1H-1，4- 二氮卓类新化合物的合 成(Ⅱ)

沈敬山;雷厉军;严铁马;韦敏;嵇汝运   

  1. 中国科学院上海药物研究所.上海(200031)
  • 发布日期:2001-08-15

Synthesis of hexahydro-1H-1,4-diazepine analogues carrying the segment of (1-arylacetamide-2-tertiaryamide) ethane (Ⅱ)

Shen Jingshan;Lei Lijun;Yan Tiema;Wei Min;Ji Ruyun   

  1. Shanghai Inst Mat Med., CAS.Shanghai(200031)
  • Published:2001-08-15

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设计并合成了2-[1-(4-(N-苯基-N-丙酰基)氨基)哌啶基]甲基-六氢-1H-1，4-二氮卓7.由3经还原、氯取代、胺取代、胺脱苄反应得到了7.7经单酰化反应得到了8.8经酰化反应后得到了11个带有(1-芳乙酰胺基-2-叔氨基)乙烷结构的六氢-1H-1，4-二氮卓类目标化合物(9a～9g,10a～10d)。

关键词: 芳基, 叔胺P, 乙烷P, 乙酰胺P, 阿片, 二氮卓, 受体, 激动素, 合成法

2-(1-(4-(N-phenyl-N-propionyl)amino)piperidyl)-hexahydro- 1H-1,4- diazepine 7 was prepared starting from 3 through reduction, chlorination, amine substitution, and debenzylation.Seven target compounds of hexahydro-1H- 1,4-diazepine analogues carrying the segment of (1-arylacetamide-2-tertiaryamide) ethane were synthesized through selective acylation and acylation of compound 7, and the four target compounds 10a～10d containing hydrophilic group of hydroxy were achieved through debenzylation of 9a, 9b,9c and 9d. These products were characterized by IR, EIMS, elementary analysis and 1^H NMR. Compounds of 9a～9d and 10a～10d were tested for their biological activities.

Key words: ARYL GROUP, ETHANE P, ACETAMIDE P, OPIUM, ACCEPTOR, KINETIN, SYNTHESIS METHODS

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