期刊
ORGANIC LETTERS
卷 19, 期 24, 页码 6610-6613出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.7b03327
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资金
- Thousand Youth Talents Plan
- Shanghai Sailing Program [17YF1424100]
- Science and Technology Commission of Shanghai Municipality [17JC1401200]
- Strategic Priority Research Program of the Chinese Academy of Sciences [XDB20000000]
Catalytic enantioselective Cu-B(pin) (pin = pinacolato) addition to N-heteroaryl-substituted followed by protonation promoted by phosphine-Cu complexes is presented. The resulting alkylboron products that contain a N-heteroaryl moiety are afforded in up to 97% yield and 99:1 enantiomeric ratio. The highly versatile C-B(pin) bond can be converted to a range of useful functional groups, delivering a variety of enantiomerically enriched building blocks that are otherwise difficult to access. The utility of this method is further demonstrated by application to a fragment synthesis of biologically active molecule U-75302. Preliminary mechanistic studies revealed that the adjacent N atom of the heterocycles plays a unique role in high reactivity and enantioselectivity.
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