A NOVEL SYNTHETIC APPROACH TO PYRROLO[2,3-D]PYRIMIDINE ANTIFOLATES

被引：29

作者：

MIWA, T

HITAKA, T

AKIMOTO, H

机构：

[1] Pharmaceutical Research Laboratories III, Pharmaceutical Research Division, Takeda Chemical Industries, Ltd., Osaka 532, 17-85, Jusohonmachi 2-chome, Yodogawa-ku

来源：

JOURNAL OF ORGANIC CHEMISTRY | 1993年 / 58卷 / 07期

关键词：

D O I：

10.1021/jo00059a016

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A novel and efficient synthetic method for the synthesis of pyrrolo[2,3-d]pyrimidine antifolates is described. The key reaction of this method is the photo-initiated free radical addition of bromomalononitrile or ethyl bromocyanoacetate to an enol ether to afford the backbone skeleton of the targeted antifolate molecule. The key intermediates 3 or 4 are smoothly converted to the pyrrolo[2,3-d]pyrimidine antifolates 1 or 2 in three steps and in high overall yield.

引用

页码：1696 / 1701

页数：6

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