INDUSTRIAL PROCESS OF MONO-ALKYLATING A PIPERIDINE NITROGEN IN PIPERIDINE DERIVATIVES WITH DEUTERATED-ALKYL

摘要

The present invention relates to a method of mono-alkylating a piperidine nitrogen in a piperidine derivative with a deuterated lower-alkyl, which comprises protecting the piperidine nitrogen with an aralkyl protective group, lower-alkylating the piperidine nitrogen with a deuterated-lower-alkylating agent under neutral or basic condition, and then deprotecting the aralkyl protective group.