Construction of a 2,6-Difunctionalized 2-Methyl-2H-l-benzopyran Library by Using a Solid-Phase Synthesis Protocol

摘要

A library containing 1200 analogues of 2,6-difunctionalized 2-methyl-2H-l-benzopyran was constructed by using a solid-phase synthesis protocol.Polymer-bound 6-amido-,6-sul-fonamido-,and 6-uredo-functionalized 2-hydroxymethyl-2-methylbenzopyrans 10 were prepared as part of a first-generation diversification step by employing reactions of respective acid halides,sulfonyl chlorides,and isocyanates with the amine precursor 7.Transformations of the resin-bound intermediates 10 by reactions with alkyl and acid halides were then used to produce a diverse series of 2,6-difunctionalized 2-methyl-2H-l-benzopyran analogues 12 and 14.