Stereospecific Suzuki−Miyaura Coupling of Chiral α-(Acylamino)benzylboronic Esters with Inversion of Configuration
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The first invertive B-alkyl Suzuki−Miyaura coupling has been achieved. The coupling of enantioenriched α-(acylamino)benzylboronic esters with aryl bromides and chlorides took place efficiently in toluene at 80 °C in the presence of Pd(dba)2 (5 mol %), XPhos (10 mol %), K2CO3 (3 equiv), and H2O (2 equiv). The reaction proceeded with inversion of configuration to give diarylmethanamine derivatives in high yields with high conservation of enantiomeric excesses.
创建时间：
2010-09-29
