American Cyanamid Company

Intervet International B.v.

Basf Se Corporation

Microbial Chemistry Research Foundation

Monika Brink

Marcus Rainer Knell

Jan Hendrik Wevers

Laurens Wilhelm Van Den Akker

Willi Heinz

Fritz Blatter

Thorsten Meyer

Timo Rager

Ralf Warrass

Hans Peter Niedermann

Stephan Veit

Meinrad Brenner

Tanja Schweisel

Kerstin Fleischhauer

Heinz-Jorg Wennesheimer

Renat Kadyrov

Gerhard Geiβ

Juan Jose Almena-Perea

Heinz-Jörg Wennesheimer

Gerhard Geiss

Guixian Hu

Marcus Knell

Heinz-Joerg Wennesheimer

This invention relates to a process for the hydrogenation of a ketooxime to selectively form an aminoalcohol stereoisomer, and, in particular, to a process for the hydrogenation of 4,5-dihydro-imidazo[4,5,1-jk][1]benzazepin-2,6,7[1H]-trione-6-oxime or a salt thereof to selectively form a stereoisomer of 6-amino-7-hydroxy-4,5,6,7-tetrahydro-imidazo[4,5,1-jk][1]-benzazepin-2[1H]-one or a salt thereof. This invention also relates to the use of the 6-amino-7-hydroxy-4,5,6,7-tetrahydro-imidazo[4,5,1-jk][1]-benzazepin-2[1H]-one hydrogenation product or a salt thereof to selectively make a stereoisomer of zilpaterol or a salt thereof, as well as the use of such a zilpaterol stereoisomer or salt in methods of treatment and medicaments for animals.

Enantioselective synthesis of 6-amino-7-hydroxy-4,5,6,7-tetrahydro-imidazo[4,5,1-jk][1]-benzazepin-2[1H]-one and zilpaterol

This invention relates to a method for making macrolides, and, in particular, a method for making optionally substituted 20,23-dipiperidinyl-5-O-mycaminosyl-tylonolide and derivatives thereof, as well as uses of macrolides to make medicaments, methods of treatment using macrolides, and methods for making intermediates that, inter alia, may be used to make macrolides. This invention also relates to solvated and non-solvated crystalline forms of 20,23-dipiperidinyl-5-O-mycaminosyl-tylonolide, as well as methods for making such crystalline forms, medicaments comprising (or derived from) such crystalline forms, methods for making medicaments comprising (or derived from) such crystalline forms, methods of treatment using such crystalline forms, and kits comprising such crystalline forms.

Macrolide synthesis process and solid-state forms

The invention relates to a process for the preparation of pyridylcarboxylic amides and esters I, Formula (I) wherein Hal, X and Rhave the meanings given in claim, which comprises the following steps: (a) heating a mixture consisting essentially of trichloromethylpyridine II, Formula (II), wherein Hal has the meaning given, and 1.0 to 1.5 equivalents of concentrated sulfuric acid, characterized in that the trichloromethylpyridine II in a liquid form is added to the concentrated sulfuric acid at a temperature from 110&#xb0; C. to 160&#xb0; C.; and (b) reacting the intermediate product obtained in step (a) with an amine or alcohol III, HXR, wherein X and Rhave the meaning given, optionally in the presence of a solvent and/or a base.

Process for the preparation of pyridylcarboxylic amides and esters

The invention relates to a process for the preparation of hetero)aryloxyheteroarylcarboxylic amide or ester of formula VI

Preparation of heteroarylcarboxamides

The invention relates to a process for the preparation of heteroarylcarboxylic amides and esters of formula I ##STR1## in which one or two of the groups A.sup.1, A.sup.2, A.sup.3, A.sup.4, and A.sup.5 represent a nitrogen atom and the other groups each independently represent CR.sup.3,

Preparation of hetero arylcarboxamides

An effective and efficient process for the preparation of chloro-benzoylchlorides of formula I, ##STR1## (n is defined in the specification). In this process a a chloro-trichloromethylbenzene of formula II ##STR2## is treated with water acid in the presence of a Lewis at temperatures below 80.degree. C. The compounds obtained according to this process can be used to prepare certain chloro-substituted benzophenones.

Process for the preparation of chloro-benzoylchlorides

Process for the preparation of chloro-benzoyl chlorides

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Ingelheim, Germany

Monika Brink