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
收藏
页码:1696 / 1701
页数:6
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