Synthesis of NB-506, a new anticancer agent

被引:57
作者
Ohkubo, M
Kawamoto, H
Ohno, T
Nakano, M
Morishima, H
机构
[1] Banyu Tukuba Research Institute, Merck Research Laboratories, Tsukuba 300-33
关键词
D O I
10.1016/S0040-4020(96)01004-6
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
6-N-formylamino-12,13-dihydro-1,11-dihydroxy-13-(beta-D-glucopyranosyl)-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7(6H)-dione (NB-506, 2), a derivative of the naturally occurring antitumor compound, BE-13793C (3), is a new indolopyrrolocarbazole anticancer agent which potently inhibits topoisomerase I. The synthesis of NB-506 was accomplished starting from dibromomaleimide 4 and indole compound 5. The key step, a glycosylation of indolocarbazole, was precisely studied to develop a practical synthesis method using KOH as a base. Copyright (C) 1996 Elsevier Science Ltd
引用
收藏
页码:585 / 592
页数:8
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