三取代1H-吡啶并[2,3-d]嘧啶-4-酮及相关杂环的通用固相合成

Versatile solid-phase synthesis of trisubstituted 1H-pyrido[2,3-d]pyrimidin-4-ones and related heterocycles.

作者信息

Schell Peter, Richards Matthew P, Hanson Kelley, Berk Scott C, Makara Gergely M

机构信息

NeoGenesis Pharmaceuticals, 840 Memorial Drive, Cambridge, Massachusetts 02139, USA.

出版信息

J Comb Chem. 2005 Jan-Feb;7(1):96-8. doi: 10.1021/cc049921m.

DOI:10.1021/cc049921m

Abstract

A solid-phase synthesis of trisubstituted 1H-pyrido[2,3-d]pyrimidin-4-ones has been developed. The synthesis utilizes solid-phase bound N-2,6-dichloronicotinoyl-1H-benzotriazole-1-carboximidamides as key intermediates. Sequential substitution of benzotriazole and the two chlorines furnishes the title compounds with regioselectivity and high purity. Application of the method to various disubstituted analogues is also demonstrated.

摘要

已开发出一种三取代1H-吡啶并[2,3-d]嘧啶-4-酮的固相合成方法。该合成方法利用固相结合的N-2,6-二氯烟酰基-1H-苯并三唑-1-甲脒作为关键中间体。苯并三唑和两个氯的顺序取代以区域选择性和高纯度提供标题化合物。还展示了该方法在各种二取代类似物中的应用。

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