Synthesis and biological activity of [Tic5] didemnin B

[摘要] A didemnin B analog containing a Tic (1,2,3,3-tetrahydroisoquinoline-3-carboxylic acid) as a conformationally restrained replacement for tyrosine has been synthesized and shown to have comparable potency as a protein biosynthesis inhibitor. Synthetic highlights include an oxidation of an alcohol to an acid in the presence of the sensitive Tic heterocycle and a modified Schmidt-type one-pot macrocyclization. (C) 1998 Elsevier Science Ltd. All rights reserved.

[发布日期] 1998-12-15