Solid-phase library synthesis of triazolopyridazines via [4+2] cycloadditions

被引：43

作者：

Boldi, AM ^{[1
]}

Johnson, CR ^{[1
]}

Eissa, HO ^{[1
]}

机构：

[1] Axys Pharmaceut Inc, S San Francisco, CA 94080 USA

来源：

TETRAHEDRON LETTERS | 1999年 / 40卷 / 04期

关键词：

D O I：

10.1016/S0040-4039(98)02449-6

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

The solid-phase library synthesis of triazolopyridazines was accomplished using a [4+2] cycloaddition strategy. The Homer-Wadsworth-Emmons (HWE) reagent diethylphosphonoacetic acid was attached to the N-terminus of amino acids on Rink amide solid-phase peptide synthesis support. The HWE reaction with a variety of alpha,beta-unsaturated aldehydes gave high conversion to diene amides. Subsequent [4+2] cycloaddition with ii-substituted urazines gave triazolopyridazines upon cleavage from resin. An alternate [4+2] cycloaddition method with urazine followed by a Mitsunobu reaction also provided triazolopyridazines. (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：619 / 622

页数：4

共 33 条

[1] THE SYNTHESIS OF UNUSUAL ORGANIC-MOLECULES FROM AZOALKANES [J].