Fine Tech Corporation

Par Pharmaceutical, Inc.

Finetech Laboratories Ltd.

Eleonora Shkolnik

Arie L Gutman

Igor Zaltzman

Genady Nisnevich

Boris Tishin

Process for making cyanomethyl ester precursors of flecainide

Process and a novel intermediate for the preparation of Flecainide

The present invention relates to a new process for the preparation of acetylcholinesterase inhibitors of formula (I) or a salt thereof, wherein: R is N-acyl-4-piperidyl; N-alkoxycarbonyl-4-piperidyl; N-alkyl-4-piperidyl; N-benzyl-4-piperidyl; N-(&ohgr;-aralkyl)-4-piperidyl; 4-pyridyl; R , R , R , and R are identical or different and each represents hydrogen, straight-chain or branched alkyl, aryl, hydroxy, alkoxy, aryloxy, benzyloxy, acyloxy, alkylthio, arylthio, benzylthio, acylamino, phthalimido or halogen; n is 1, 2 or 3; m is 1, 2, 3, 4, or 5. This process comprises cyclisation of a compound of formula (II) or salts thereof, wherein R , R , R , R and R , m and n are as defined above; R is selected from a derivatised or non-derivatised carboxyl, cyano, N-substituted aminocarbonyl groups or hydrogen; R is selected from a derivatised or non-derivatised carboxyl, cyano or N-substituted aminocarbonyl groups, optionally in the presence of acids and/or solvents. One of the most potent acetylcholinesterase inhibitors of the class of compounds prepared according to the present invention is donepezil.

Process and intermediates for production of donepezil and related compounds

Process for the preparation of flecainide

A process for producing trifluoroethoxybenzoic acids or salts thereof by reaction of halobenzoic acids or salts thereof with 2,2,2-trifluoroethanol in the presence of a strong base and copper containing materials. The compounds obtained by the process of the present invention may be used as synthetic intermediates in the pharmaceutical industry.

Process for the preparation of (2,2,2-trifluoroethoxy)benzoic acids

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Nesher, Israel

Eleonora Shkolnik