Solid phase synthesis of sulfahydantoins

被引：22

作者：

Albericio, F

Garcia, J

Michelotti, EL

Nicolás, E

Tice, CM

机构：

[1] Rohm & Haas Co, Spring House, PA 19477 USA

[2] Univ Barcelona, Dept Organ Chem, E-08028 Barcelona, Spain

来源：

TETRAHEDRON LETTERS | 2000年 / 41卷 / 17期

关键词：

amino acids; combinatorial chemistry; cyclitive cleavage; libraries; thiadiazoles;

D O I：

10.1016/S0040-4039(00)00321-X

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A five step solid phase synthesis of 2-unsubstituted 1,2,5-thiadiazolidin-3-one 1,1-dioxides (sulfahydantoins) from N-alpha-FMOC-amino acids and aromatic aldehydes is described. The key step is the base mediated cyclitive cleavage of a resin bound N-alpha-(aminosulfonyl)-N-alpha-benzyl-amino acid to afford the desired product. This synthesis allows the preparation of a diverse library of compounds based on this heterocycle. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：3161 / 3163

页数：3

共 29 条

[1] SYNTHESIS AND CYCLIZATION OF CARBOXYLSULFAMIDES DERIVED FROM AMINO-ACIDS [J].