Janssen Pharmaceutica Nv

Cilag International Gmbh

Stefan Horns

Susanne Lochner

Matteo Conza

Magali B Hickey

Diego Broggini

Thomas Bader

Frank Ralf Porstmann

Zhaobin Wang

Lucie Lovelle

Oliver Flögel

Guangrong Tang

Neelakandha S Mani

Daniel J Pippel

Luigi Anzalone

Penina Feibush

Roger Faessler

Ilias Konstantinos Dorziotis

Frank J Villani, Jr

The present invention relates to certain intermediates useful in the preparation of certain benzoimidazol-2-yl pyrimidines and processes for preparing them. In particular, the present invention relates to various 2-[3-(1-methyl-piperidin-4-yl)-propylamino]-pyrimidine-5-carboxylic acids and amides as useful intermediates in the preparation of compounds including 

Substituted 2-[3-(1-methyl-piperidin-4-yl)-propylamino]-pyrimidine-5-carboxylic acids and amides and methods of making the same

Benzoimidazol-2-yl pyrimidines, purification methods for the same, and pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by Hreceptor activity, including allergy, asthma, autoimmune diseases, and pruritus.

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The present invention is directed to an improved process for the preparation of sulfamide derivatives.

Process for the preparation of sulfamide derivatives

Benzoimidazol-2-yl pyrimidine modulators of the histamine h4 receptor

The present invention relates to a process for isolating (&#x3b1;S,&#x3b2;R)-6-bromo-&#x3b1;-[2-(dimethylamino)ethyl]-2-methoxy-&#x3b1;-1-naphthalenyl-&#x3b2;-phenyl-3-quinolineethanol from a mixture of stereoisomeric forms of 6-bromo-&#x3b1;-[2-(dimethylamino)ethyl]-2-methoxy-&#x3b1;-1-naphthalenyl-&#x3b2;-phenyl-3-quinolineethanol by optical resolution with chiral 4-hydroxydinaphtho[2,1-d:1',2&#x2032;-f][1,3,2]dioxaphosphepin 4-oxide or a derivative thereof, in particular (11bR)-4-hydroxydinaphtho[2,1-d:1&#x2032;,2&#x2032;-f][1,3,2]dioxaphosphepin 4-oxide, as resolution agent.

Process for preparing (alpha S, beta R)-6-bromo-alpha-[2-(dimethylamino)ethyl]-2- methoxy-alpha-1-naphthalenyl-beta-phenyl-3-quinolineethanol

The present invention is directed to an improved process for synthesizing phosphonic and phosphinic acid chymase inhibitor compounds.

Process for synthesizing phosphonic and phosphinic acid compounds

The present invention relates to a process for isolating (&#x3b1;S,&#x3b2;R)-6-bromo-&#x3b1;-[2-(dimethylamino)ethyl]-2-methoxy-&#x3b1;--naphthalenyl-&#x3b2;-phenyl-3-quinolineethanol from a mixture of stereoisomeric forms of 6-bromo-&#x3b1;-[2-(dimethylamino)ethyl]-2-methoxy-&#x3b1;-1-naphthalenyl-&#x3b2;-phenyl-3-quinolineethanol by optical resolution with chiral 4-hydroxydinaphtho[2,1-d:1',2&#x2032;-f][1,3,2]dioxaphosphepin 4-oxide or a derivative thereof, in particular (11bR)-4-hydroxydinaphtho[2,1-d:1&#x2032;,2&#x2032;-f][1,3,2]dioxaphosphepin 4-oxide, as resolution agent.

Process for preparing (alpha S, beta R)-6-bromo-alpha-[2-(dimethylamino) ethyl]-2-methoxy-alpha-1-naphthalenyl-beta-phenyl-3-quinolineethanol

N-ethyl-N-[3-(3-cyanopyrazolo[1,5-a]pyrimidine-7-yl)phenyl]acetamide (Zaleplon) can be produced by condensing 3-(N-acetyl-N-ethyl-amino)-&#x3b2;-oxo-phenylpropanal sodium salt with 3-amino-4-cyanopyrazole. Said sodium salt can be produced by first treating 3-acetylamino-acetophenone with an alkali metal hydroxide, in particular with powdered potassium hydroxide and then with an ethylating reagent, in particular ethyl bromide and the N-(3-acetylphenyl)-N-ethyl-acetamide that is obtained is reacted with a formic acid alkyl ester in the presence of an alkali metal alkanolate, in particular in the presence of sodium ethanolate. Zaleplon is the active ingredient of the soporific licensed under the trade name Sonata&#xae;.

Method for producing n-ethyl-n-[3-(3-cyanopyrazolo[1,5a]pyrimidine-7-yl)phenyl]acetamide

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Schaffhausen, Switzerland

Stefan Horns