
Tetrahedron Asymmetry p. 1673 - 1679 (1999)
Update date:2022-08-03
Topics: Aldehydes Regioselectivity Lewis acid Yield Steric hindrance Enantiomeric excess (ee) Nucleophilic addition coordination complex Chelation Catalytic asymmetric synthesis Chiral Ligands Substrate Scope Chiral Auxiliary Enantioselective Addition Transition state Optical activity Stereocenter
Shi, Min
Jiang, Jian-Kang
Chiral C2-symmetric 2,4-disubstituted azetidine derivatives having a β-amino alcohol moiety have been successfully synthesized and their stereoselective catalytic abilities have been examined in the asymmetric addition of diethylzinc to aldehydes in hexane. When N-(2,2-diphenyl-2- hydroxyethyl)-(S,S)-2,4-bis(methoxymethyl)azetidine 12 was used as a catalytic chiral ligand, the production of sec-alcohols having an S-absolute configuration could be achieved in high chemical yields (92-99%) and high enantiomeric excesses (83-93% for arylaldehydes and 63-65% for aliphatic aldehydes). For some arylaldehydes, the enantioselectivities are higher than the corresponding chiral C2-symmetric 2,5-disubstituted pyrrolidine ligands. However, when the chiral C2-symmetric azetidine derivatives 13 and 14, which have bulky substituents on the 2,4-positions were used as the chiral ligands under the same reaction conditions, the enantiomeric excesses of the corresponding sec-alcohols decreased to 20-30%.
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Doi:10.1039/P29800000181
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(2016)