首页> 外国专利> NOVEL PROCESSES FOR THE PREPARATION OF PHENYLCYCLOPROPYLAMINE DERIVATIVES AND USE THEREOF FOR PREPARING TICAGRELOR

NOVEL PROCESSES FOR THE PREPARATION OF PHENYLCYCLOPROPYLAMINE DERIVATIVES AND USE THEREOF FOR PREPARING TICAGRELOR

机译:制备苯并环丙胺衍生物的新方法及其在制备替卡瑞洛中的应用

摘要

Provided herein are novel processes for the preparation of phenylcyclopropylamine derivatives, which are useful intermediates in the preparation of triazolo[4,5-d]pyrimidine compounds. Provided particularly herein are novel, commercially viable and industrially advantageous processes for the preparation of a substantially pure ticagrelor intermediate, trans-(1R,2S)-2-(3,4-difluorophenyl)-cyclopropylamine. Provided further herein are novel acid addition salts of trans-(1R,2S)-2-(3,4-difluorophenyl)-cyclopropylamine, and process for their preparation. The intermediate and its acid addition salts are useful for preparing ticagrelor, or a pharmaceutically acceptable salt thereof, in high yield and purity.
机译:本文提供了用于制备苯基环丙胺衍生物的新颖方法,其是用于制备三唑并[4,5-d]嘧啶化合物的有用中间体。本文特别提供了新颖的,商业上可行的和工业上有利的方法,用于制备基本上纯的替卡格雷或中间体反式-(1R,2S)-2-(3,4-二氟苯基)-环丙胺。本文进一步提供了反式-(1R,2S)-2-(3,4-二氟苯基)-环丙胺的新型酸加成盐及其制备方法。中间体及其酸加成盐可用于以高产率和纯度制备替卡格雷或其药学上可接受的盐。

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