PRODUCTS OF CHIRAL SYNTHESIS OF CIS-IMIDAZOLINE COMPOUNDS AND THEIR USE

    公开(公告)号:US20190270726A1

    公开(公告)日:2019-09-05

    申请号:US16415862

    申请日:2019-05-17

    摘要: This invention provides a method for enantioselective synthesis of cis-imidazolines and related structures through chiral resolution. A chiral acid is used to separate enantiomeric precursors of the cis-imidazolines from a racemic mixture by selective crystallization. Both enantiomers can be cyclized into the desired cis-imidazoline by complementary pathways. Compounds can be synthesized according to the invention with an enantiomeric excess as high as 99%. Cis-imidazolines such as Nutlin-3a prepared according to this invention may be used for treating cancer, killing senescent cells, or treating senescence-associated conditions.

    Chiral synthesis method for producing cis-imidazoline compounds for pharmaceutical use

    公开(公告)号:US10329279B2

    公开(公告)日:2019-06-25

    申请号:US15955474

    申请日:2018-04-17

    摘要: This invention provides a method for enantioselective synthesis of cis-imidazolines and related structures through chiral resolution. A chiral acid is used to separate enantiomeric precursors of the cis-imidazolines from a racemic mixture by selective crystallization. Both enantiomers can be cyclized into the desired cis-imidazoline by complementary pathways. Compounds can be synthesized according to the invention with an enantiomeric excess as high as 99%. Cis-imidazolines such as Nutlin-3a prepared according to this invention may be used for treating cancer, killing senescent cells, or treating senescence-associated conditions.