Blaschim S.p.a.

Ravizza S.p.a.

Biaschim S.p.a.

Oreste Piccolo

Ermanno Valoti

Giovanni Villa

Giuseppina Visentin

Enrico Zen

Attilio Citterio

Ambrogio Magni

Aldo Belli

Alberto Verga

Franca Spreafico

Pietro Blasina

Antonio Ascheri

The keto group at the 7-position of a bile keto acid is stereoselectively reduced to a beta-hydroxy group with hydrogen in the presence of nickel, a base (the quantity of which is at least 0.3 mole for each mole of keto acid), and an alcohol having from 3 to 10 C atoms, selected from the group consisting of secondary alcohols, tertiary alcohols and beta-branched alcohols.

Stereoselective reduction of the keto group at 7-position of a bile keto

Process for preparing Naproxen via a sequence of stereospecific reactions which comprises: condensation of 1-chloro-2-methoxy-naphthalene with a (S)-2-halo-propionyl halide according to the Friedel-Crafts reaction, ketalization of the thus obtained (S)-2-halo-1-(5'-chloro-6'-methoxy-2'-naphthyl)-propan-1-one, rearrangement of said ketal to afford an ester, hydrolysis of the ester and removal of the chlorine atom in 5-position by hydrogenolysis. New (S) 2-halo-1-(5'-chloro-6'-methoxy-2'-naphthyl)-propan-1-ones.

Process for preparing naproxen

A process for the resolution of (.+-.) 2-[2'-(p-fluorophenyl)-5'-benzoxazolyl]-propionic acid, indicated for brevity as (.+-.)-FBP, by treatment with (-)N-R-glucamine, indicated for brevity as NRG and in which R is an alkyl or cycloalkyl radical, followed by fractional crystallization of the mixture of the diastereoisomer salts obtained, and by separation of the precipitate, from which, by hydrolysis, (.+-.)-FBP is obtained with the required purity characteristics. The levorotatory antipode, (-)-FBP, is racemized, preferably by the formation of one of its esters, which is then hydrolyzed to give the (.+-.)-FBP, which is recycled to the treatment with NRG. (+)-FBP and (-)-FBP salts with NRG obtained by said process.

Process for the resolution of (.+-.)

Preparation of aryl alkyl ketones by reaction of an aryl compound with an aliphatic acid and/or a functional derivative thereof in anhydrous hydrofluoric acid.

Process for the preparation of aryl alkyl ketones

Process for the optical resolution of (.+-.)2-(6'methoxy-2'-naphthyl)-propionic acid by adding from 0.45 to 0.65 mole of (S)-alpha-phenylethylamine to each mole of said acid in chloroform.

Process for the optical resolution of

Improvement in the process for preparing biaryl compounds via coupling of an arylamine with an arene in the presence of a nitrite, an acid and copper metal or a derivative thereof; the improvement is consisting in adding to the reaction mixture a trialkylorthoformate. The process may be used for preparing drugs such as Flurbiprofen and Xenbucin or intermediate compounds particularly useful for preparing Flurbiprofen, Flufenisal, Chlordimorin, Xenbucin, Xenysalate, Xenyhexenic acid and the like.

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Leghorn, Italy

Oreste Piccolo