期刊
JOURNAL OF ORGANIC CHEMISTRY
卷 77, 期 24, 页码 11296-11301出版社
AMER CHEMICAL SOC
DOI: 10.1021/jo302406w
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资金
- Engineering and Physical Sciences Research Council (EPSRC) Pharma Synthesis Programme
- GlaxoSmithKline
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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