Janssen Pharmaceutica Nv

Michel Joseph Maurice André Guillaume

Yolande Lydia Lang

Stefan Marcel Herman Leurs

Dirk De Smaele

Georges Joseph Cornelius Hoornaert

Armin Roessler

Frans Josef Cornelius Compernolle

Bart Petrus Anna Maria Jozef Medaer

Tomasz Kozlecki

Jozef Ludo Jan Cuypers

Hua Mao

Ivan Joseph Maria Vervest

Tim Gaekens

Lars Ulmer

Thierry Brossette

Dirk Janssen Pharmaceutica NV De Smaele

Armin Cilag Ag Pharmaceutical & Chem Roessler

The present invention relates to a novel process, suitable for industrial exploitation for the production of N-(2,6-dimethyl-phenyl)-2-piperazin-1-yl-acetamide, also known as N-lidocaine, obtained from the reaction of piperazine with N-haloacetyl-2,6-xylidine. The process comprises the consecutive steps a) through f)

Process for the production of n-(2,6-dimethyl-phenyl)-2-piperazin-1-yl-acetamide

The present invention relates to ester prodrugs of nalmefene of formula (I), pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of substance abuse disorders such as alcohol abuse and alcohol dependence and impulse control disorders such as pathological gambling and addiction to shopping. 

Nalmefene prodrugs

The present invention concerns the use of dibutyl tin oxide for regioselective catalytic diol mono-tosylation at a concentration lower than 2 mol %. The present invention also concerns the use of a generic acetal compound of Formula (Ic) in a catalytic process for regioselective diol mono-tosylation, wherein Y is selected from the group of Calkyl, phenyl and benzyl. The concentration of the generic acetal compound of Formula (Ic) is less than about 2 mol %, preferably ranges between about 2 mol % and about 0.0005 mol %, preferably ranges between about 0.1 mol % and about 0.005 mol %. 

Process for regioselective mono-tosylation of diols

The present invention relates to a novel process for the production of [2-(4-fluoro-benzyl)-phenyl]-acetic acid, a compound obtainable from phthalic anhydride. The process comprises the subsequent steps a) through e): In an alternative embodiment, the step e) is replaced by the steps f1) and f2): The present invention provides a process for the production of [2-(4-fluoro-benzyl)-phenyl]-acetic acid which is suitable for industrial scale reactors (e.g. which is cleaner and more efficient). Also, [2-(4-fluoro-benzyl)-phenyl]-acetic acid is obtained as a crystalline material with a purity &#x3e;95%.

Process for the production of [2-(4-fluoro-benzyl)-phenyl]-acetic acid

The present invention concerns processes for the preparation of each of the 4 diastereomers of formula (I)in stereochemically pure form from either of two enantiomerically pure precursors. The tetracyclic ringsystem having trans-fused five and seven membered rings is formed in an acid-catalysed cyclization reaction. The invention further relates to the thus obtained cis-fused tetracyclic alcohol intermediates, the methanamine end-products, the methanamine end-products for use as a medicine, in particular as CNS active medicines.

Preparation of trans-fused 3,3a,8,12b-tetrahydro-2h-dibenzo[3,4:6,7]cyclohepta[1,2-b]furan derivatives

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Berg, Belgium

Michel Joseph Maurice André Guillaume