Egis Gyogyszergyar Rt.

Egis Gyogyszergyar Nyilvanosan Mukodo Reszvenytarsasag

Budapesti Vegyimuvek

János Szulágyi

Gyula Simig

Tibor Mezei

József Barkóczy

Ferenc Bihari

Peter Bohus

Balázs Volk

Márta Porcs-Makkay

Kálmán Nagy

Gyula Eifert

Gyula Lukács

Istvan Kuronya

Györgyi Vereczkeyné Donáth

Enikó Molnár

Gábor Berecz

Marianna Kertesz Nee Szabo

Gyuláné Körtvélyessy

György Clementis

Peter Boros

József Reiter

Jeno Meszaros

László Pongó

Péter Slégel

László Koncz

Mária Vajjon

Enikö Molnár

Agnes Meszaros Nee Szekrenyes

Odon S Jartoo

Laszlo Gondos

Jószef Barkóczy

The invention relates to a process for the preparation of cyclopropyl benzyl ketone compounds of formula (II) wherein Rrepresents fluorine or chlorine atom or Calkoxy group, by the reaction of a Grignard reagent, obtained from the reaction of compound of formula (V), wherein X represents chlorine or fluorine atom, with the compound of formula (IV), wherein Rrepresents Calkyl group, having a straight or branched chain. The process can be applied preferably on industrial scale. Compound of formula (II), wherein R represents a fluorine atom in position 2 is an intermediate of the preparation process of prasugrel, which is a platelet inhibitor used in the therapy. 

Process for the preparation of pharmaceutical intermediates

The invention relates to a process for the preparation of 3-{2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl}-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one of the Formula (I), and pharmaceutically acceptable acid addition salts thereof by subjecting the oxime of the Formula (II), to ring-closure in the presence of an alkali hydroxide, alkali carbonate or alkali-Calkoxide in an inert organic solvent, converting the base of the Formula I thus obtained into an acid addition salt or setting free the base of the Formula I from an acid addition salt thereof which comprises reacting a halogen derivative of the general Formula (XIV), (wherein Hal is halogen) with piperidine oxime derivative of the Formula (V), or an acid addition salt thereof in the presence of a base, and using by the ring-closure of the oxime of the Formula II formed a C-alkanol as inert solvent. The process of the present invention enables the economical preparation of a product having a purity suitable for pharmaceutical purposes.

Process for the preparation of 3-{2-'4- (6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyllethyl}-6,7,8,9-tetrahydro-2-methyl-4h-pyrido&#x2032;1,2-methyl-4h-pyrido&#x2032;,2-a!pyrimidin-4-one

According to the present invention there are provided fungicidal compositions comprising as active ingredient in an amount of 0.01-80% by weight a new benzoic acid derivative of the general Formula I ##STR1## wherein R.sub.1 and R.sub.2 stand for hydrogen, C.sub.1-8 alkyl, C.sub.2-8 alkenyl or benzyl;

Benzoic acid derivatives

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Budapest, Hungary

János Szulágyi