- Preparation method of chiral 3-substituted pyrrolidine derivative
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The invention provides a preparation method of a chiral 3-substituted pyrrolidine derivative. The preparation method comprises an intermediate preparation step, a diastereomer mixture preparation step, a chiral separation step and a chiral 3-substituted pyrrolidine derivative synthesis step. According to the invention, through catalytic asymmetric kinetic resolution, a mixture of two diastereoisomers is efficiently converted into a diastereoisomer with a certain single configuration, chiral separation is realized, a key intermediate is obtained with high yield, and a series of chiral 3-substituted pyrrolidine derivatives are synthesized. The whole reaction route is mild in reaction condition, simple and convenient to operate, high in resolution efficiency, high in atom economy, low in costand suitable for industrial scale production.
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- KRAS G12C INHIBITORS
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The present invention relates to compounds that inhibit KRas G12C. In particular, the present invention relates to compounds that irreversibly inhibit the activity of KRas G12C, pharmaceutical compositions comprising the compounds and methods of use therefor.
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Paragraph 0755
(2017/12/18)
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