Sanofi-a Ventis Deutschland Gmbh

Aventis Pharmaceuticals Inc.

Reda Hanna

Heinz-Werner Kleemann

Gerrit Schubert

Joerg Rieke-Zapp

Bao-Guo Huang

Yves Gouraud

Johannes Keil

Xiao-Dong Wu

Nicholas J Hrib

Brian S Freed

John G Jurcak

John D Tomer, Iv

James Hendrix

George Lee

Gregory Shutske

Franz J Weiberth

Juergen Mueller-Lehar

Silke Dubberke

Roland Utz

The present invention relates to processes for preparing (3-oxo-2,3-dihydro-1H-isoindol-1-yl)acetylguanidine derivatives of the formula I via 3-hydroxy-2,3-dihydro-1H-isoindol-1-one derivatives or 3-(2-carbamoylphenyl)-acrylic ester derivatives as intermediates, to a process for optical resolution, and to intermediates of the process according to the invention.

Process for preparing (3-oxo-2,3-dihydro-1H-isoindol-1-yl) acetylguanidine derivatives

A method and apparatus for preventing board warpage during the application and curing or drying of liquid epoxies, or the like, on printed circuit boards using a clamping fixture assembly, which includes at least one clamping fixture support and at least one clamping fixture overlay. If desired, a plurality of printed circuit boards may be processed using an appropriate clamping fixture assembly. Furthermore, the clamping fixture may be constructed so a slight bow or curvature thereof can counter either a convex or concave bow or curvature of the printed circuit board. In the method, at least one printed circuit board is mounted to a clamping fixture support whereby a clamping fixture overlay is placed on top of the first printed circuit board.

The compounds are of the class of benzisoxazolyl-, pyridoisoxazolyl- and benzthienyl-phenoxy derivatives, useful as Dantagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of Dreceptor. These conditions comprise, for example, Attention Deficit Hyperactivity Disorder, Obsessive-Compulsive Disorder, Psychoses, Substance Abuse, Substance Dependence, Parkinson's Disease, Parkinsonism, Tardive Diskinesia, Gilles de la Tourette Syndrome, Conduct Disorder, and Oppositional Defiant Disorder. A further aspect of the invention is to provide a pharmaceutical composition, intermediates, and a method of making said class of compounds.

[object Object]

An improved process for the preparation of N-amino nitrogen heterocyclic compounds is disclosed and claimed. In an embodiment of this invention, a compound of the formula (VI) is prepared starting from the corresponding indole derivative by way of N-amination and subsequently forming an hydrazone by the reaction with a keto compound in a single step. Further reduction of the hydrazone and subsequent coupling with a pyridine compound affords the compound of formula VI or a suitable salt thereof. 

Process for the preparation of N-amino substituted heterocyclic compounds

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Allentown, PA, United States of America

Reda Hanna