申请人:Han Zhengxu
公开号:US20050165240A1
公开(公告)日:2005-07-28
This invention provides a method of preparing amine stereoisomers, which comprises stereoselectively reducing a sulfinylimine that bears on the sulfinyl group a residue of an alcohol, thiol or amine, or reacting a sulfinylimine stereoisomer that bears on the sulfinyl group a residue of an alcohol, thiol or amine with a source of a nucleophile, to afford a sulfinylamine stereoisomer, followed by contacting the sulfinylamine stereoisomer with a reagent suitable for the cleavage of a sulfur-nitrogen bond, to afford an amine stereoisomer. It also provides novel intermediates useful in the method, and the use of certain of the intermediates in the preparation of sulfoxide and sulfinylamine stereoisomers.
本发明提供了一种制备胺立体异构体的方法,包括选择性地还原带有醇、硫醇或胺残基的亚磺酰亚胺,或将带有醇、硫醇或胺残基的亚磺酰亚胺立体异构体与核苷酸源反应,得到亚磺酰胺立体异构体,然后将亚磺酰胺立体异构体与适用于断裂硫-氮键的试剂接触,得到胺立体异构体。本发明还提供了在该方法中有用的新型中间体,以及某些中间体在制备亚砜和亚磺酰胺立体异构体中的使用。