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首页> 外国专利> PROCESS FOR THE PREPARATION OF PHENYL ALANINE DERIVATIVES WITH CHINAZOLINDION CRUISES, AND INTERMEDIATE PRODUCTS FOR THE MANUFACTURE

PROCESS FOR THE PREPARATION OF PHENYL ALANINE DERIVATIVES WITH CHINAZOLINDION CRUISES, AND INTERMEDIATE PRODUCTS FOR THE MANUFACTURE

机译：具有中国唑啉巡航导弹的苯丙氨酸衍生物的制备方法及其中间体产品

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摘要

A method for preparing a phenylalanine derivative having a quinazoline-dione ring represented by the following formula (1) or a pharmaceutically acceptable salt thereof, comprising the following steps (a), (b) and (c): (a) reacting an acyl phenylalanine derivative represented by the following formula (2): with a carbonyl group-introducing reagent and a specific anthranilic acid derivative to thus form the corresponding carboxy-asymmetric urea derivative; (b) converting the carboxy-asymmetric urea derivative into the corresponding quinazoline-dione derivative in the presence of a carboxyl group-activating agent: (c) if desired, substituting an N-alkyl group for the hydrogen atom bonded to the nitrogen atom present in the quinazoline-dione ring of the quinazoline-dione derivative using an N-alkylation agent and then deprotecting the resulting product, when the substituent R3' which is a group corresponding to R3 is protected. According to this method, there can be obtained a phenylalanine derivative having a quinazoline-dione skeleton in a industrially favorably high yield.
机译：一种具有下式（1）表示的具有喹唑啉-二酮环的苯丙氨酸衍生物或其药学上可接受的盐的制备方法，其包括以下步骤（a），（b）和（c）：（a）使下式（2）表示的酰基苯丙氨酸衍生物反应：与引入羰基的试剂和特定的邻氨基苯甲酸衍生物形成相应的羧基不对称脲衍生物。（b）在羧基活化剂的存在下将羧基不对称脲衍生物转化为相应的喹唑啉二酮衍生物：（c）如果需要，使用N-烷基化剂，用N-烷基取代与存在于喹唑啉-二酮衍生物的喹唑啉-二酮环上的氮原子键合的氢原子，然后当取代基被脱保护时，保护所得产物。作为与R3相对应的基团的R3′被保护。根据该方法，可以以工业上有利的高收率获得具有喹唑啉-二酮骨架的苯丙氨酸衍生物。

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