Accessing chiral 2,2-disubstituted morpholines via organocatalytic enantioselective chlorocycloetherification
ORGANIC CHEMISTRY FRONTIERS(2022)
摘要
Chiral morpholine is an important scaffold in organic synthesis and a pharmacophore in medicinal chemistry. However, catalytic enantioselective procedures for the construction of morpholines remain sparse. We report herein a catalytic asymmetric halocyclization protocol to furnish morpholines containing a quaternary stereocenter using cinchona alkaloid-derived phthalazine as the catalyst. Various chlorinated 2,2-disubstituted morpholines are achieved from alkenol substrates in excellent yields and enantioselectivities under mild conditions.
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关键词
organocatalytic enantioselective chlorocycloetherification,morpholines
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