Lonza Ag

Lonza Inc.

Other

Merck + Co., Inc.

Yves Bessard

Jean-Paul Roduit

Gerhard C Stucky

James Edward Leresche

Josef Heveling

Erich Armbruster

Ralf Proplesch

David Kuo

A four-step process for preparing 1-(6-methylpyridin-3-yl)-2-[4-(methylsulfonyl)phenyl]ethanone of the formula: starting from 2-methyl-5-ethylpyridine. 1-(6-Methylpyridin-3yl)-2-[4-(methylsulfonyl)phenyl]ethanone is an intermediate for preparing inhibitors.

Process for preparing 1-(6-methylpyridin-3-yl)-2-[4- (methylsulphonyl)phenyl]ethanone

A starting product for the preparation of COX-2 inhibitors, notably the compound 1-(6-methylpyridine-3-yl)-2-[(4-(methylsulfonyl)phenyl]ethanone of the formula (I): A method for making the compound.

1-(6-methylpyridine-3-yl)-2-[4-(methylsulphonyl) phenyl] ethanone and method for its preparation

A method for preparing pyridine-2,3-dicarboxylic acid esters of the general formula:wherein R is C-alkyl, C-cycloalkyl, aryl or arylalkyl, and Rto R, independently of one another, represent hydrogen, C-alkyl, fluorinated C-alkyl, C-alkoxy, (C-alkoxy)-C-alkyl or (C-alkoxy)carbonyl. These esters are obtained from the corresponding 2,3-dichloropyridine, the corresponding alcohol ROH and carbon monoxide in the presence of a palladium-diphosphine complex and a weak base. Pyridine-2,3-dicarboxylic acid esters are herbicides or intermediates for the preparation of herbicides.

Method for preparing pyridine-2,3-dicarboxylic acid esters

Process for preparing 1-(6-methylpyridin-3-yl)-2-&lsqb;4-(methylsulfony)phenyl&rsqb;ethanone

Process for preparing 1-(6-methylpyridin-3-yl)-2-&lsqb;4-methylsulphonyl)-phenyl&rsqb;ethanone

A new process for the catalytic conversion of hydroxymethyl imidazoles to formylimidazoles is described. The reaction takes place in the presence of a peroxide. Formylimidazoles are important intermediate products for pharmaceutical substances.

Procedure for producing formylimidazoles

A new procedure for the catalytic conversion of hydroxy methyl imidazoles to formyl imidazoles is described. The catalysis takes place in the presence of a peroxide. Formyl imidazoles are important intermediate products for pharmaceutical substances.

Procedure for producing formyl imidazoles

A process for preparing pyridinecarboxylic esters of the general formula:

Process for preparing pyridinecarboxylic esters

A process for preparing pyridinecarboxylic esters of the general formula: ##STR1## wherein R.sup.1 is hydrogen, a C.sub.1 -C.sub.6 -alkyl group, a C.sub.1 -C.sub.4 -alkoxycarbonyl group or a C.sub.1 -C.sub.4 -alkoxymethyl group, R.sup.2 is a C.sub.1 -C.sub.4 -alkyl group and X is chlorine or bromine. The pyridinecarboxylic esters are obtained by reacting the corresponding 2,3-dihalopyridines with carbon monoxide and a C.sub.1 -C.sub.4 -alkanol in the presence of a weak base and a complex of palladium with a bis(diphenylphosphine). Pyridinecarboxylic esters are intermediates for preparing herbicides and drugs against fibrotic diseases.

A process for the preparation of 2,6-pyridinedicarboxylic acid esters of the general formula: ##STR1## wherein R.sup.1 is a C.sub.1 -C.sub.6 -alkyl group, a C.sub.3 -C.sub.6 -cycloalkyl group, an aryl group or an arylalkyl group, and R.sup.2 and R.sup.3 independently of one another are hydrogen or chlorine and R.sup.4 is hydrogen, a C.sub.1 -C.sub.6 -alkyl group, a C.sub.1 -C.sub.6 -alkoxy group or fluorine. The 2,6-pyridinedicarboxylic acid esters are obtained by reaction of the corresponding halopyridines with carbon monoxide and an alcohol of the general formula:

Process for the preparation of 2,6-pyridinedicarboxylic acid esters

A process for preparing 2-pyrimidinecarboxylates of the general formula: ##STR1## wherein R is C.sub.1-6 -alkyl, C.sub.3-6 -cycloalkyl, aryl or arylalkyl, and R.sup.1 to R.sup.3 are, independently of one another, hydrogen, C.sub.1-6 -alkyl, fluorinated C.sub.1-6 -alkyl, C.sub.1-6 -alkoxy, (C.sub.1-6 -alkoxy)-C.sub.1-6 -alkyl or (C.sub.1-6 -alkoxy)carbonyl. These are obtained from the corresponding 2-halopyrimidine, the corresponding alcohol ROH and carbon monoxide in the presence of a palladium/phosphine complex and a base. 2-pyrimidinecarboxylates are intermediates for preparing herbicides.

Process for preparing 2- pyrimidinecarboxylates

A novel process for the preparation of substituted pyrimidine derivatives of the general formula: ##STR1## in which a halopyrimidine is reacted in the presence of a sulfinate with a compound selected from the series: ##STR2## The compounds of the general formula I are precursors of, for example, compounds with herbicidal activity.

Process for the preparation of substituted pyrimidines

A method for preparing pyrimidin-2-ylacetic acid esters of the general formula: ##STR1## wherein R is C.sub.1-6 -alkyl, C.sub.3-6 -cycloalkyl, aryl or arylalkyl and R.sup.1 to R.sup.3, independently of one another, are hydrogen, C.sub.1-6 -alkyl, fluorinated C.sub.1-6 -alkyl, C.sub.1-6 -alkoxy, (C.sub.1-6 -alkoxy)-C.sub.1-6 -alkyl or (C.sub.1-6 -alkoxy)carbonyl. These esters are obtained from the corresponding 2-(halomethyl)-pyrimidine, the corresponding alcohol ROH and carbon monoxide in the presence of a palladium-phosphine complex and a base. Pyrimidin-2-ylacetic acid esters are intermediates in the preparation of herbicides.

Growing community of inventors

Sierre, Switzerland

Yves Bessard