Schering Corporation

Ingrid Mergelsberg

Jacques Gosteli

Dinesh Gala

Brigitte Giesinger

Anantha R Sudhakar

William W Leong

Martin Steinman

David R Andrews

Richard W Draper

Donald Hou

Gary M Lee

Janet L Mas

Markus Tanner

Frank Guenter

Dominik Scherer

Process for preparing N-(4-hydroxyphenyl)-N&prime;-(4&prime;-aminophenyl)-piperazine

Aminomethyl-phenylimidazoles are produced by reaction of an ester of a hydroxymethyl-phenylimidazole with an amine. A particularly preferred ester is the acetate ester. The aminomethyl-phenylimidazoles have useful properties as highly selective partial agonists or antagonists at brain dopamine receptor subtypes. A preferred compound prepared is 5-fluoro-2-�4-�(2-phenyl-1H-imidazol-5-yl)methyl!-1-piperazinyl!pyrimidine . Esters of the hydroxymethyl-phenylimidazoles are useful intermediates.

Preparation of aminomethyl-phenylimidazoles

Described is a process for preparing triazolone compounds of the formula ##STR1## comprising heating a mixture of a compound of the formula ##STR2## and a hydrazine derivative of the formula R.sup.5 --NH--NH--CHO, R.sup.5 --NH--NH--C(O)OC(CH.sub.3).sub.3 or R.sup.5 --NH--NH--C(O)OCH.sub.2 C.sub.6 H.sub.5, optionally in the presence of an added base.

Process for the preparation of triazolones

Disclosed are a process and intermediates of the formulae ##STR1## wherein X.sup.- is halide, BF.sub.4.sup.-, R.sup.3 SO.sub.3.sup.-, wherein R.sup.3 is C.sub.1 -C.sub.6 alkyl, CF.sub.3, C.sub.1 -C.sub.6 alkylphenyl or phenyl, and Q is a group of the formula ##STR2## wherein R is C.sub.1 -C.sub.6 alkyl; useful for preparing benzazepine intermediates of the formula ##STR3## These benzazepine intermediates are useful for preparing benzazepines having activity as selective D1 receptor antagonists.

Process for preparing benzazepine intermediates for the synthesis of D1

Diastereoselective process for preparing n-substituted amino acids and

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Dagmersellen, Switzerland

Ingrid Mergelsberg