Approaches for the Synthesis of Functionalized Cryptophycins

作者:Sammet Benedikt; Bogner Tobias; Nahrwold Markus; Weiss Christine; Sewald Norbert*
来源:Journal of Organic Chemistry, 2010, 75(20): 6953-6960.
DOI:10.1021/jo101563s

摘要

The first syntheses of bioactive cryptophycins functionalized at unit ID were accomplished ina one-pot Staudinger reduction/cyclization step An a/ado precursor for the lower part of the backbone was introduced to minimize protective group chemistry and enable a very convenient synthesis of cryptophycin-52 and unit D eryptophycin analogues containing an ester or a free carboxylic acid for bioconjugations Both new cryptophycin derivatives show high biological activity in cytotoxicity assays

  • 出版日期2010-10-15