[EN] INDUSTRIAL PROCESS OF MONO-ALKYLATING A PIPERIDINE NITROGEN IN PIPERIDINE DERIVATIVES WITH DEUTERATED-ALKYL<br/>[FR] PROCÉDÉ INDUSTRIEL DE MONOALKYLATION D'UN AZOTE DE PIPÉRIDINE DANS DES DÉRIVÉS DE LA PIPÉRIDINE AVEC UN ALKYLE DEUTÉRÉ
申请人:OTSUKA PHARMA CO LTD
公开号:WO2019049918A1
公开(公告)日:2019-03-14
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.
本发明涉及一种用氘代低烷基对哌啶衍生物中的哌啶氮进行单烷基化的方法,包括用芳基保护基保护哌啶氮,使用氘代低烷基化试剂在中性或碱性条件下对哌啶氮进行低烷基化,然后去除芳基保护基。