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Ucb Pharma Gmbh

Seth C Ennis

Claus Meese

Ralf Kanzler

Roland Drews

Cornelia Fuchs

Dean A Johnson

Bryan D Kennedy

This disclosure relates to process for the preparation of a compound of formula (I) wherein R is hydrogen, a straight or branched C-Calkyl-carbonyl 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)&#x2014;LiY wherein n is 1 or 2; Ris 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 C-Calkyl 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. 

Accelerated synthesis of substituted hydroxymethyl phenols

The present disclosure relates to a process for the preparation of a compound of formula (I) wherein R is hydrogen, a formyl group, a straight, branched or cyclic C-Calkylcarbonyl group or a phenylcarbonyl group, or a salt thereof, characterized by the steps of reacting a compound of formula (II) with a mixture of Grignard initiator and Mg in a solvent to form a Grignard reagent, reacting the Grignard reagent with paraformaldehyde or trioxane to obtain a compound of formula (III) and then further reacting the compound of formula (III) in a known manner to obtain a compound of formula (I) and optionally salt formation. 

Shortened synthesis using paraformaldehyde or trioxane

The present invention provides a process for the production of a compound of formula (I) or a salt thereof, wherein R is hydrogen, a straight, branched or cyclic C-Calkyl group or an aryl group which may optionally be substituted. This process comprises: (a) reacting a compound of formula (II), with a compound of formula (III), wherein R is as defined above and X is a leaving group, in the presence of N,N-di-isopropylethylamine. 

Synthesis of phenolic esters of hydroxymethyl phenols

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Limerick, Ireland

Seth C Ennis