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1. 发明授权

US4793948A Bile acid derivatives and production thereof 失效
标题翻译：胆汁酸衍生物及其生产
公开(公告)号：US4793948A
公开(公告)日：1988-12-27
申请号：US7663
申请日：1987-01-28
申请人： Shunsou Hatono , Akira Yazaki , Susumu Yoshida
发明人： Shunsou Hatono , Akira Yazaki , Susumu Yoshida
IPC分类号： A61K31/575 , C07J41/00 , C07J1/00
CPC分类号： A61K47/48123 , C07J41/0055 , C07J41/0061
摘要： A bile acid derivative having carcinostatic activity represented by the following formula (1): ##STR1## wherein each of R.sub.1 and R.sub.2 is a hydrogen atom or a hydroxyl group, R.sub.3 is a hydroxyl group, benzyloxyl group or --NH--CH.sub.2n R.sub.5 (wherein R.sub.5 is a carboxyl group or sulfonyl group, and n represents the integer of 1 or 2), X is a halogen atom, R.sub.4 is a hydrogen atom or XCH.sub.2 CH.sub.2 --,.chi. is an .alpha.-bond, and .chi. is an .alpha.- or .beta.-bond is produced by the steps (a) and (b), the steps (a), (b) and (c), or the steps (a), (b), (c) and (d) described below:(a) causing an active carbonation reagent to react with a bile acid derivative wherein the carboxyl group is esterified;(b) causing an aminoalkylhalide to react with the active carbonated product obtained;(c) subjecting the bile acid derivative obtained in the above steps (a) and (b) to hydrolysis; and(d) causing the above hydrolyzate to react with an aminoalkyl derivative in the presence of a condensing agent.
摘要翻译：具有由下式（1）表示的具有制癌活性的胆汁酸衍生物：其中R1和R2各自为氢原子或羟基，R3为羟基，苄氧基或-NH-CH2nR5 （其中R5是羧基或磺酰基，n表示1或2的整数），X是卤素原子，R4是氢原子或XCH2CH2-，chi是α键，chi是α - 或（b），步骤（a），（b）和（c），或步骤（a），（b），（c）和（d）（a）使活性碳酸化试剂与其中羧基被酯化的胆汁酸衍生物反应; （b）使氨基烷基卤化物与得到的活性碳酸化产物反应; （c）将上述步骤（a）和（b）中获得的胆汁酸衍生物进行水解; 和（d）使上述水解产物在缩合剂存在下与氨基烷基衍生物反应。

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