Smithkline Corporation

Smithkline Beckman Corporation

Bing L Lam

Lendon N Pridgen

George R Wellman

Robert L Webb

Wilford L Mendelson

Joseph J Lewis

Elvin L Anderson

Charles B Spainhour, Jr

This invention relates to substituted 4-pyrimidinones which are useful as intermediates in preparing H.sub.2 -antagonists.

Substituted pyrimidinones

A series of chemical reactions starting from the condensation of uracil with an acid stable heterocyclic aldehyde in an acid medium produces biologically active end products which are 2-heterocyclylmethylthioethylamino-5-heterocyclylmethyl-4-pyrimidinones. The new reactions and intermediates of this invention are particularly useful for preparing 2[2-(5-dimethylaminomethyl-2-furylmethylthio)-ethylamino]-5-(6-methyl-3-py ridylmethyl)-4-pyrimidinone and its salts. This compound is a potent H.sub.2 -antagonist with a long duration of activity.

Chemical methods and intermediates for preparing substituted

Intermediates for preparing substituted pyrimidinones

A process for preparing 3-chloro-6-(2-hydroxyphenyl)pyridazines by the reaction of 6-(2-hydroxyphenyl)-3(2H)-pyridazinones with phosphorus oxychloride and a disubstituted formamide. The chloropyridazine compounds are useful intermediates for preparing compounds which have .beta.-adrenergic blocking and vasodilator activity and are useful as antihypertensive agents.

Process for preparing 3-chloro-6-(2-hydroxyphenyl)-pyridazines

A method for preparing 1,2,3,4-tetrahydroisoquinolines comprising heating N-halo or hydroxyethyl-N-benzylamines in an aluminum chloride melt at 160.degree.-210.degree..

Method for preparing tetrahydroisoquinolines

A process for preparing 5-(alkoxy- and aminoethylthio)methylthiazole compounds via displacement of the trisubstituted phosphonium group from 5-(trisubstituted phosphonium)methylthiazole compounds is disclosed.

Process for preparing 5-(alkoxy- and aminoethyl thio)methylthiazole

A method of preparing .alpha.,.beta.-epoxy ketones by reacting water-soluble .alpha.,.beta.-ethylenic ketones with sodium hypochlorite. Especially useful for preparing 3,4-epoxy-butanone.

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King of Prussia, PA, United States of America

Bing L Lam