Solid phase synthesis of 1-alkyl-2-alkylthio-5-carbamoylbenzimidazoles

被引：75

作者：

Lee, J ^{[1
]}

Gauthier, D ^{[1
]}

Rivero, RA ^{[1
]}

机构：

[1] RW Johnson Pharmaceut Res Inst, Spring House, PA 19447 USA

来源：

TETRAHEDRON LETTERS | 1998年 / 39卷 / 3-4期

关键词：

D O I：

10.1016/S0040-4039(97)10525-1

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

The preparation of 1-alkyl-2-alkylthio-5-carbamoylbenzimidazoles 7 is described. The cyclization of a resin bound o-phenylenediamine 4 with thiocarbonyldiimidazole (TCD) in THF provided a benzimidazole-2-thione 5. Treatment of 5 with benzylic halides in the presence of DIEA resulted in the resin bound 1-alkyl-2-alkylthio-5-carbamoylbenzimidazoles 6. The final products were cleaved from the resin and obtained in from 74% to 99% yields. (C) 1997 Elsevier Science Ltd. All rights reserved.

引用

页码：201 / 204

页数：4

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