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Highly Enantioselective addition of in situ prepared Arylzinc to Aldehydes catalyzed by a series of Atropisomeric Binaphthyl-Derived Amino Alcohols

机译:一系列对映异构体联萘衍生的氨基醇催化原位制备的芳基锌对醛的高度对映选择性

摘要

The direct addition of in situ prepared arylzinc to aldehydes with chiral binaphthyl-derived amino alcohols as catalysts can afford optically active diarylmethanols in high yields and with excellent enantioselectivities (up to 99 % ee, ee=enantiomeric excess). By using a single catalyst, both enantiomers of many pharmaceutically interesting diarylmethanols can be obtained by the proper combination of various arylzinc reagents with different aldehydes; this catalytic system also works well for the phenylation of aliphatic aldehydes to give up to 96 % ee.
机译:用手性联萘衍生的氨基醇作为催化剂直接将原位制备的芳基锌加到醛中,可以以高收率和优异的对映选择性(高达99%ee,ee =对映体过量)提供光学活性的二芳基甲醇。通过使用单一催化剂,可以通过将各种芳基锌试剂与不同的醛适当组合来获得许多药学上有意义的二芳基甲醇的两种对映异构体。该催化体系也能很好地用于脂族醛的苯基化反应,从而产生高达96%的ee。

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