Usv Pharmaceutical Corporation

Merck + Co., Inc.

The Dupont Merck Pharmaceutical Company

Rorer Pharmaceutical Corporation

Science Union Et Cie

Joseph Auerbach

Frederick A Golec, Jr

Lin-Hua Zhang

Fu-chih Huang

Steven A Weissman

Martin L Kantor

Robert S Hoerrner

Martin Kantor

John Carolan

Protriptyline can be prepared from 5-dihydrodibenzocycloheptatriene, by deprotonation, followed by reaction at low temperatures with 1,3-bromochloropropane to give the 5-(chloropropyl)-dibenzocycloheptatriene, which is reacted with methylamine in a displacement reaction to give the protriptyline product.

Process for preparing dibenzocycloheptene compounds

This invention relates to compounds, including 5-chloro-2-[2-[[(4-methylphenyl)sulfonyl]oxy]ethyl]-7-[2,4,6-trimethylphen yl)methoxy]anthra[1,9-cd]pyrazol-6(2H)-one and analogs thereof, which are useful as intermediates for the synthesis of anthrapyrazolone anticancer agents, including losoxantrone. This invention also relates to methods for the synthesis of anthrapyrazolone anticancer agents, including losoxantrone.

Method for the synthesis of anthrapyrazolones

Intermediates for the synthesis of anthrapyrazolone anticancer agents

4-Substituted-1,4-dihydropyridines are prepared by a cycloaddition reaction in which the cyclization is driven to completion, after thermal reaction, by addition of an acid. Felodipine, a vasodilator, is prepared by a cycloaddition reaction of ethyl 3-aminocrotonate with a suitably substituted dichlorobenzylidine under reaction conditions whereby the product crystallizes out of the reaction solution and may be directly isolated by filtration.

Process for the preparation of 4-substituted-1,4-dihydropydrines

A novel procedure for bromination of aromatic moieties utilizes N-bromosuccinimide or dibromodimethylhydantoin in an aqueous alkali medium. The bromination procedure is employed for the preparation of an intermediate used in the preparation of remoxipride, an antipsychotic compound.

Process for aromatic bromination

This invention relates to new lipoxygenase inhibitors possessing anti-inflammatory and anti-allergic properties. The present new compounds are of the formula: ##STR1## and salts thereof; wherein, R is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower aralkyl, phenyl, naphthyl, or a nitrogen oxygen or sulfur heterocyclic; and

Aryl pyrroles as useful antiallergy compounds

Provided are new compounds having valuable therapeutic activity. These compounds are of the formula: ##STR1## and salts thereof, wherein

Aryl-alkyl heterocyclic compounds

Compounds of the structure ##STR1## wherein R is hydrogen, lower alkyl containing 1 to 5 carbon atoms, cycloalkyl containing 3 to 7 carbon atoms, phenyl or phenyl substituted with halogen, trifluoromethyl, or lower alkyl or lower alkoxy having 1 to 4 carbon atoms and R.sub.1 is hydrogen, lower alkyl having 1 to 4 carbon atoms, phenyl or phenyl lower alkyl wherein the lower alkyl has 1 to 4 carbon atoms, are formed by cyclizing a compound of the structure ##STR2## wherein R and R.sub.1 are as defined above, in the presence of an acid.

Process for synthesizing certain N-benzoylamino indolines

The process of preparing a compound of the formula: ##STR1## wherein, Y and Z are each H, alkyl, halo, alkoxy, trifluoromethyl, hydroxy, alkanoyloxy, or alkanoylamino;

Process for forming certain substituted phthalimidines

Compounds of the formula ##STR1## wherein, Y and Z are each H, alkyl, halo, alkoxy, trifluoromethyl, hydroxy, alkanoyloxy, or alkanoylamino;

Intermediates for the synthesis of phthalimidines

Compounds of the formula ##STR1## wherein: Ar and Ar' are independently alicyclic aryl or heterocyclic aryl groups;

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Brooklyn, NY, United States of America

Joseph Auerbach