首页> 外国专利> Optically active or racemic bromine - 14 - oxo - e - homoeburnanderivate process for manufacturing the same and of optically active or racemic 11 - bromvincaminsaeureesterderivaten and optically active or racemic 11 - bromvincaminsaeureesterderivate as well as the former or the latter, drugs containing

Optically active or racemic bromine - 14 - oxo - e - homoeburnanderivate process for manufacturing the same and of optically active or racemic 11 - bromvincaminsaeureesterderivaten and optically active or racemic 11 - bromvincaminsaeureesterderivate as well as the former or the latter, drugs containing

机译：-光学活性或外消旋的溴-14-氧代-e-同型异戊二烯酸酯化方法，用于制造相同的光学活性或外消旋的11-溴香豆素氨基脲酸酯和光学活性或外消旋的11-溴香豆素氨基脲酸酯以及前者或后者，含有

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摘要

A novel process for preparing 11-bromo-vincaminic acid esters of the general formula ##STR1## wherein R.sup.1 and R.sup.2 each stand independently from each other for a C.sub.1-6 alkyl group, comprising the steps of treating a 1-alkyl-1-alkoxycarbonylethyl-octahydroindolo- quinolisine of the general formula ##STR2## wherein R.sup.2 is as defined above and R.sup.3 stands for a C.sub.1-6 alkyl group, with a brominating agent and treating the resulting isomeric mixture of the bromo- derivatives with an alkaline agent or treating the corresponding 14-oxo-E- homo-eburnane being unsubstituted in ring A with a brominating agent and nitrosating the resulting 11-bromo-14-oxo-E-homo-eburnane of the general formula ##STR3## wherein R.sup.2 is as defined above, then subjecting the resulting 11-bromo-14-oxo-15-hydroxyimino-E-homoeburnanes to deoxyimination and treating the 14,15-dioxo-derivatives obtained with a base in an alcohol of the general formula R.sup.1 OH, wherein R.sup.1 is as defined above.PPAll the intermediate products are novel and exhibit a therapeutical protecting effect against cerebral hypoxy.

机译：制备通式为## STR1 ##的11-溴-烟酰胺酸酯的新方法，其中R.sup.1和R.sup.2彼此独立地代表C.sub.1-6烷基，其包括处理通式为## STR2 ##的1-烷基-1-烷氧基羰基乙基-八氢吲哚并喹啉的步骤，其中Rsup 2如上定义，Rsup 3代表C。 1-6烷基，用溴化剂处理，然后用碱性试剂处理溴衍生物的异构体混合物，或用溴化剂处理环A中未取代的相应的14-氧代-E-均-丁烷，并亚硝化得到的通式为## STR3 ##的11-溴-14-氧代-E-均-丁烷，其中R 2如上所定义，然后使所得的11-溴-14-氧代-15-羟基亚氨基- E-高纯烷烃用于脱氧和处理由碱在通式R.sup.1 OH的醇中获得的14,15-二氧代衍生物，其中R.sup.1如上定义ve.P

所有中间产物都是新颖的，并且表现出针对脑缺氧的治疗保护作用。展开▼

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公开/公告号DE2928187A1

专利类型
公开/公告日1980-01-24

原文格式PDF
申请/专利权人 RICHTER GEDEON VEGYESZET;
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申请/专利号DE19792928187
发明设计人 DANCSI LAJOS DIPL CHEM;KEVE TIBOR DIPL CHEM DR;KARPATI EGON DR;SZANTAY CSABA DIPL ING CHEM DR;SZPORNY LASZLO DR;SZABO LAJOS DIPL CHEM DR;KALAUS GYOERGY DIPL ING CHEM D;
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申请日1979-07-12
分类号C07D471/22;A61K31/475;
国家 DE
入库时间 2022-08-22 17:31:09

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