Accelerated synthesis of (3-Diisopropylamino-1-phenylpropyl)-4-(hydroxymethyl)phenol and its phenolic monoesters

摘要

This disclosure relates to process for the preparation of a compound of formula (I):- wherein R is hydrogen, a straight or branched C1-C6 alkylcarbonyl group or a phenylcarbonyl group, or a salt thereof, comprising the following steps: (a) adding to a suspension of Mg a compound of formula (II) R?? (MgX)nÀ LiY (II), wherein n is 1 or 2; R is an aromatic, aliphatic, carbocyclic or heterocyclic organic group having 1 to 24 carbon atoms; X and Y are independently selected from Cl, Br and I; (b)reacting said reaction mixture with a suitable halogenated compound in a solvent to form a Grignard reagent; (c) reacting said Grignard reagent with a suitable linear, branched or cyclic carbonate to obtain a compound of formula (IV):- , wherein A is a linear, branched or cyclic C1-C6 alkyl group, and preferably a methyl group, and then further reacting the compound of formula (IV) in a known manner to obtain a compound of formula (I) and optionally salt formation.