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JOURNAL ARTICLE
RESEARCH SUPPORT, NON-U.S. GOV'T
Total synthesis of resorcinol amide Hsp90 inhibitor AT13387.
Journal of Organic Chemistry 2012 December 22
The synthesis of C-5-substituted resorcinol amide AT13387, a known Hsp90 inhibitor currently in clinical trials, is reported without the use of phenolic protection in an overall yield of 13.4%. Biomimetic aromatization and Suzuki-Miyaura cross coupling approach were employed to synthesize the resorcinol and iso-indoline units, respectively, which were efficiently coupled using Grignard-mediated amidation.
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