Solid-phase combinatorial synthesis of 1,4-benzoxazin-3(4H)-one and 1,4-benzothiazin-3(4H)-one derivatives

被引：31

作者：

Lee, CL ^{[1
]}

Chan, KP ^{[1
]}

Lam, YL ^{[1
]}

Lee, SY ^{[1
]}

机构：

[1] Natl Univ Singapore, Dept Chem, Singapore 117543, Singapore

来源：

TETRAHEDRON LETTERS | 2001年 / 42卷 / 06期

关键词：

solid-phase synthesis; 1,4-benzothiazin-3(4H)-one; 1,4-benzoxazin-3(4H)-one;

D O I：

10.1016/S0040-4039(00)02199-7

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

The first solid-phase synthesis of 1,4-benzothiazin-3(4H)-ones and 1,4-benzoxazin-3(4H)-ones is reported. Alkylation of the immobilized 4-hydroxy-3-nitrobenzamide 2a and 3-nitro-4-sulfanylbenzamide 2b, followed by reduction and cyclization gave 4. Further alkylation and acylation was performed on the amide nitrogen in the presence of sodium hydride followed by TFA cleavage to give the desired 1,4-benzothiazin-3(4H)-ones and 1,4-benzoxazin-3(4H)-ones. (C) 2001 Elsevier Science Ltd. All rights reserved.

引用

页码：1167 / 1169

页数：3

共 18 条

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