期刊
ORGANIC LETTERS
卷 20, 期 4, 页码 971-974出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.7b03878
关键词
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资金
- National Natural Science Foundation of China [21202092]
- Project of Scientific Research of Hubei Provincial Education Department [B2016024]
- China Three Gorges University [KJ2014H008, KJ2014B084]
- Yichang Humanwell Pharmaceutical Co., Ltd. [SDHZ2015003]
A highly enantioselective transfer hydrogenation of non-ortho-substituted aryl N-heteroaryl ketones, using readily available chiral diamine-derived iridium complex (S,S)-1f as a catalyst and sodium formate as a hydrogen source in a mixture of H2O/i-PrOH (v/v = 1:1) under ambient conditions, is described. The chiral aryl N-heteroaryl methanols were obtained with up to 98.2% ee by introducing an N-oxide as a removable ortho-substituent. In contrast, no more than 15.1% ee was observed in the absence of an N-oxide moiety. Furthermore, the practical utility of this protocol was also demonstrated by gram-scale asymmetric synthesis of bepotastine besilate in 51% total yield and 99.9% ee.
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