Journal
CHEMICAL COMMUNICATIONS
Volume 56, Issue 3, Pages 423-426Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c9cc08795h
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Funding
- Guangzhou key laboratory of construction and application of new drug screening model systems [201805010006]
- key laboratory of new drug discovery and evaluation of ordinary universities of Guangdong province [2017KSYS002]
- Guangdong Pharmaceutical University [51377002]
- Youth Innovation Talents Project of Colleges and Universities in Guangdong Province [51377201]
- Natural Science Foundation of Hunan Province [12019JJ60071]
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Iridium-catalyzed boron-hydrogen bond insertion reactions of trimethylamine-borane and sulfoxonium ylides have been demonstrated, furnishing alpha-boryl ketones in moderate to excellent yields in most cases (51 examples; up to 84%). This practical and scalable insertion reaction showed broad substrate scope, high functional-group compatibility and could be applied in late-stage modification of structurally complex drug compounds. Further synthetic applications were also demonstrated.
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