首页> 外国专利> A PROCESS FOR MONO-N-BETA HYDROXYLATION OF CYCLENE FOR THE PRODUCTION OF A N-BETA-HYDROXYALKYL-1, 4, 7, 10-TETRAAZACYCLODODECANE

A PROCESS FOR MONO-N-BETA HYDROXYLATION OF CYCLENE FOR THE PRODUCTION OF A N-BETA-HYDROXYALKYL-1, 4, 7, 10-TETRAAZACYCLODODECANE

机译:用于单环-N-BET羟基氧化的环化反应过程,用于生产N-BETA-羟基烷基-1,4,7,10-四氮杂双环十二烷

摘要

A process for mono-N-beta hydroxylation of cyclene for the production of a N-beta-hydroxyalkyl-l, 4, 7, 10-tetraazacyclododecane of formula I where Rl is and R2 and R3 are, iadependently of one another, a hydrogen atom, together with the carbon atoms they are bonded to a 4-, 5-, 6-or 7-niembered cycloalkyl ring which optionally can be interrupted by 1 to 3 oxygen atom(s), or a C1-C12 alkyl radical which optionally is substituted with 1 to 3 C1-C6 alkyl groups or 1 to 3 hydroxy groups, whereby the optionally present hydroxyl radicals are optionally present in protected form, which comprises reacting 1,4,7, 10-tetraazacyclodecane, optionally in the form of a salt, with, an epoxide of formula 11, in which R2 and R3 have the above-indicated meanings, in the presence of 0.8-1.1 mol of lithium salt relative to one mol of cyclene at a temperature of from 40-150°C, and working up the reaction in aqueous form.
机译:一种用于生产环戊烯的单N-β-羟基化方法,用于制备式I的N-β-羟基烷基-1、4、7、10-四氮杂环十二烷,其中R1是且R2和R3彼此独立地是氢原子与碳原子一起键合至4、5、6或7位的环烷基环上,该环烷基环可任选被1-3个氧原子或C1-C12烷基基团打断被1至3个C 1 -C 6烷基或1至3个羟基取代,由此任选存在的羟基以受保护的形式任选存在,其包括使1,4,7,10-四氮杂环癸烷反应,任选地以在40-150°C的温度下,相对于1 mol环戊烯,在0.8-1.1 mol锂盐的存在下,具有式11的环氧化物的盐,其中R2和R3具有上述含义,并以水性形式进行反应。

著录项

  • 公开/公告号IN1998DE01436A

    专利类型

  • 公开/公告日2009-03-20

    原文格式PDF

  • 申请/专利权人

    申请/专利号IN1436/DEL/1998

  • 发明设计人 PETER BLASZKIEWICZ;ORLIN PETROV;

    申请日1998-05-28

  • 分类号A61K31/41;

  • 国家 IN

  • 入库时间 2022-08-21 19:27:38

相似文献

  • 专利
  • 外文文献
  • 中文文献
获取专利

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号