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A reaction sequence involving the chemoselective olefinic oxidation of N(1)-benzyl-2,7-dihydro-1H-azepine with m-CPBA in the presence of HBF(4) and BnOH followed by ring contraction facilitates the stereoselective preparation of either of the epoxide diastereoisomers of (2RS,3SR)-N(1)-benzyl-2-chloromethyl-3-benzyloxy-4,5-epoxypiperidine by simple modification of the reaction conditions. Epoxide ring opening, functional group interconversion, and deprotection allow the synthesis of (+/-)-1-deoxynojirimycin and (+/-)-1-deoxyaltronojirimycin.

Original publication

DOI

10.1021/ol902533b

Type

Journal article

Journal

Org Lett

Publication Date

01/01/2010

Volume

12

Pages

136 - 139

Keywords

1-Deoxynojirimycin, Azepines, Catalysis, Crystallography, X-Ray, Molecular Conformation, Molecular Structure, Oxidation-Reduction, Stereoisomerism