Isochem

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Didier G Wirth

Claude Gueremy

Dominique Gibert

Marcel Deglave

Marc-Henri Mouton

Maurice Auclair

Laurence Ferrucio

Robert Labey

Process for preparation of a polymorphic form of terphenadine having a

2,3,5-(4H)-Trimethyl pyranone having the formula: ##STR1## which is prepared by acetylation of a ketone derived from 2-formyl-3-pentanone and preparation of 2,3,5-(1H)-trimethyl 4-pyridinone having the formula: ##STR2## by ammonolysis of the 2,3,5-(4H)-trimethyl 4-pyranone.

Pyranone, process for its preparation, its use in the preparation of a

Phenothiazine derivatives are described of the formula ##SPC1## In which X.sub.1 and X.sub.2, which may be the same or different, are H, R, F, Cl, Br, OR, CN, --COR, CH.sub.3, --S--R, --SOR, --SO.sub.2 R or --SO.sub.2 N(CH.sub.3).sub.2, where R is an alkyl group having from 1 to 4 carbon atoms, and the quinuclidine ring is substituted by the group --(CH.sub.2).sub.x -- in the 2- or 3- position, x being 1 or 2 when said group is substituted in the 2-position and being 0 or 1 when said group is substituted in the 3-position (because of electronic hindrance), and their acid addition and quaternary ammonium salts, have valuable pharmacological properties. In particular, these compounds have anti-histaminic, anti-cholinergic, adrenolytic, neuro-sedative, tranquillizing and/or spasmolytic properties. These compounds are prepared by condensing an appropriate phenothiazine with a quinuclidine derivative of the formula ##SPC2## In which x has the above-stated meaning and Z is a halogen atom or a reactive ester group.

Phenothiazine derivative

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Didier G Wirth