Chemi S.p.a.

Recordati Industria Chimica E Farmaceutica S.p.a.

Angela Tuozzi

Stefano Turchetta

Lorenzo De Ferra

Pietro Massardo

Elio Ullucci

Angelo Gentile

Franca Segnalini

Stefano Tur{overscore (c)}hetta

A process for the resolution of racemic tetrahydropapaverine with optically active arylpropionic acids is described.

Process for the resolution of isoquinoline derivatives

The present invention relates to a process for the preparation of Montelukast and the salts thereof comprising the following steps: (a) reaction of a compound A with a compound A in which n varies between 1 and 2 and, when n is 1, R is methyl and, when n is 2, R is a C-Calkyl or an aryl, and X is a leaving group, by nucleophilic substitution reactions in dipolar organic solvents to yield the compound A3 (b) reaction of the compound A3 with an inorganic acid HY, in which Y is Cl, Br, I, and subsequent isolation of the resultant salt A4; (c) optional conversion of the salt A4 into the compound A3;(d) methylation of the salt A4 and/or of the compound A3 to yield Montelukast.

Process for the preparation of Montelukast

Process for preparing sulfinyl derivatives of Formula 2, useful as inhibitors of gastric acid secretion, comprising the selective oxidation of the corresponding sulfides of formula 1, as represented in the following scheme  The oxidation is performed with hydrogen peroxide in the presence of low amounts of a rhenium compound as catalyst, at a temperature from 0&#xb0; C. to room temperature.

Process for the preparation of sulphinyl derivatives by oxidation of the corresponding sulfides

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Rome, Italy

Angela Tuozzi