期刊
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
卷 -, 期 -, 页码 5007-5016出版社
AMER CHEMICAL SOC
DOI: 10.1021/jacs.2c09958
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We have developed an enantioconvergent approach to chiral N-heterocycles using racemic diols and primary amines via cost-effective borrowing hydrogen annulation. The discovery of a chiral amine-derived iridacycle catalyst was crucial for achieving high efficiency and enantioselectivity in the one-step formation of two C-N bonds. This catalytic method provides quick access to a diverse range of enantioenriched pyrrolidines, including key precursors for valuable drugs like aticaprant and MSC 2530818.
We present an enantioconvergent access to chiral N-heterocycles directly from simple racemic diols and primary amines, through a highly economical borrowing hydrogen annulation. The identification of a chiral amine-derived iridacycle catalyst was the key for achieving high efficiency and enantioselectivity in the one-step construction of two C-N bonds. This catalytic method enabled a rapid access to a wide range of diversely substituted enantioenriched pyrrolidines including key precursors to valuable drugs such as aticaprant and MSC 2530818.
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