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1. (WO2018050546) IMPROVEMENTS IN OR RELATING TO ORGANIC MATERIAL

Pub. No.:    WO/2018/050546    International Application No.:    PCT/EP2017/072532
Publication Date: Fri Mar 23 00:59:59 CET 2018 International Filing Date: Fri Sep 08 01:59:59 CEST 2017
IPC: C07D 211/60
Applicants: UNIVERSITÉ DE LIÈGE
Inventors: MONBALIU, Jean-Christophe
GERARDY, Romaric
Title: IMPROVEMENTS IN OR RELATING TO ORGANIC MATERIAL
Abstract:
The invention provides a method for the preparation of an intermediate for use in synthesizing a lower alkyl phenidate compound of formula (I), wherein each R1 independently represents an optionally substituted aryl, heteroaryl, alkyl, cycloalkyl, alkoxy, aryloxy, acyl, carboxyl, hydroxyl, halogen, amino, nitro, sulfo or sulfhydryl group, R2 represents a hydrogen atom or a lower alkyl group, n represents an integer from 1 to 5 and m represents an integer from 1 to 3 or a pharmaceutically acceptable salt thereof; which method comprises the steps of: (a) flowing a tosylhydrazone compound of formula (IV), wherein R1, n and m are as defined above in relation to the methylphenidate of formula (I), an organic base and an organic solvent into a fluidic network; and (b) reacting the tosylhydrazone compound of formula (IV) and the base in the fluidic network under thermal and/or photochemical conditions to form a transient diazoamide compound of formula (V), wherein R1, n and m are as defined above in relation to the methylphenidate of formula (I).