
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%.
View MoreSHANGHAI T&W PHARMACEUTICAL CO., LTD.
website:http://www.trustwe.com
Contact:+86-21-61551413
Address:601, No. 1, 2277 Nong, Zu Chongzhi Road, Zhangjiang Hightech. Park, Pudong
Contact:+86-27-85733560
Address:NO.308,QINGNIAN RD.,WUHAN,CHINA
Contact:0027-717-456976
Address:2ND FLOOR, 325 VAUSE ROAD, OVERPORT, 4001, SOUTH AFRICA
Xinji City Taida Sinopec Co., Ltd.
Contact:0086-311-85341278
Address:No.6, Nanhua Road,Xinji City Road,Hebei Province,China
SHANDONG AONA CHEMICAL CO.,LTD.
Contact:86-532-85762926
Address:LIUYUAN TOWN, ZAOZHUANG CITY, SHANGDONG PROVINCE.
Doi:10.1039/P29800000181
(1980)Doi:10.1002/asia.201500854
(2016)Doi:10.1021/ol7021142
(2007)Doi:10.1021/jm00295a022
(1970)Doi:10.1002/jhet.5570360330
(1999)Doi:10.1080/17415993.2016.1166225
(2016)