Sandoz Gmbh

Newron Pharmaceuticals S.p.a.

Erwin Waldvogel

Gustav Schwarb

Claudio Giordano

Eugen Eichenberger

Jean-Pierre Bourquin

Jean-Michel Bastian

Wolfgang Skranc

Michael Wolberg

Matthias Riepl

Christoph Imboden

The present invention relates to a new process for the production of substituted 2-[2-(phenyl) ethylaminojalkaneamide derivatives of the following formula (I), in particular 2-[2-(3-butoxyphenyl)-ethylamino]-N,N-dimethylacetamide in high yields with very high chemical purity. The invention relates to a process for preparing a compound of formula (I) or a pharmaceutically acceptable salt thereof:

Process for the production of substituted 2-[2-(phenyl) ethylaminojalkaneamide derivatives

The invention relates to a new process for the production and/or purification of the salt of the compound (S)-2-[4-(2-fluorobenzyloxy) benzylamino]propanamide, i.e. ralfinamide, or the respective R-enantiomer, with methane sulfonic acid in high yields and very high enantiomeric and chemical purity in the form of the crystalline anhydrous polymorph identified as form A, wherein said salt is substantially free from impurities having genotoxic effect, such as (C-C)alkanylmethanesulfonates, and residual solvents known as potential precursors thereof, such as (C-C)alkanols or esters thereof with lower alkanoic acids.

Process for the production of ralfinamide salts substantially free from impurities having genotoxic effects

The invention relates to a new process for the production and/or purification of the salt of the compound (S)-2-[4-(2-fluorobenzyloxy) benzylamino]propanamide, i.e. ralfinamide, or the respective R-enantiomer, with methane sulfonic acid in high yields and very high enantiomeric and chemical purity in the form of the crystalline anhydrous polymorph identified as form A, wherein said salt is substantially free from impurities having genotoxic effect, such as (C1-C5)alkanylmethanesulfonates, and residual solvents known as potential precursors thereof, such as (C1-C5)alkanols or esters thereof with lower alkanoic acids.

The invention discloses a novel process for the preparation of a compound of formula II ##STR1## wherein R.sub.1 is C.sub.1-5 alkyl,

Intermediates for pyrazolyl acetic acid derivatives

The invention discloses a novel process for the preparation of a compound of formula II ##STR1## wherein R.sub.1 is C.sub.1-5 alkyl, R.sub.2 is hydrogen or C.sub.1-5 alkyl, and R.sub.3 is optionally substituted phenyl, comprising the reaction of a 4-hydroxypyrazole of formula III ##STR2## wherein R.sub.1 and R.sub.2 are as defined for formula II, with a benzylhalide of formula IV

The present invention provides anti-9,10-dihydro-4-(1-methyl-4-piperidylidene)-4H-benzo[4,5]-cyclohepta[1 ,2-b]thiophen-10(9H)-one oxime of formula ##STR1## useful for the treatment of allergic conditions.

Anti-allergic

The present invention concerns a novel process for the production of known benzocycloheptathiophene derivatives of the formula: ##STR1## wherein R.sub.1 is hydrogen, chlorine, bromine or alkoxy, and R.sub.2 is alkyl. The compounds are useful as specific histaminolytics for use in the treatment of allergic conditions.

Precursors of

The present invention concerns a novel process for the production of known benzocycloheptathiophene derivatives of the formula: ##SPC1## Wherein R.sub.1 is hydrogen, chlorine, bromine or alkoxy, and R.sub.2 is alkyl. The compounds are useful as specific histaminolytics for use in the treatment of allergic conditions.

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Aesch, Switzerland

Erwin Waldvogel