Pfizer Corporation

Other

Brian C Vanderplas

Frank J Urban

Keith Michael DeVries

Ravi Mysore Shanker

Dennis Michael Godek

Charles W Murtiashaw

Jeffrey W Raggon

Takushi Kaneko

Jotham Wadsworth Coe

Stanton F McHardy

William Thomas McMillen

Derek Lawrence Tickner

John Anthony Ragan

Robert W McLaughlin

David H B Ripin

This present invention relates to a new and improved reductive amination process for the preparation of 3-azabicyclo[3.1.0]hexane derivatives and pharmaceutical compositions comprising such derivatives. The invention particularly relates to using such derivatives to treat certain disorders and conditions, including, for example, irritable bowel syndrome, drug addiction or dependency, alcohol addiction or dependency, depression, and eating disorders.

Preparation of 3-azabicyclo [3.1.0] hexane derivatives

Synthesis of carbamate ketolide antibiotics

The instant invention relates to intermediates of Formula II, ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined in the specification, and to processes for preparing such intermediates. This invention also relates to processes for preparing compounds of Formula III, ##STR2## and enantiomers thereof, wherein R.sup.2, R.sup.3 and R.sup.4 are as defined in the specification. Compounds of Formula II and Formula III are intermediates in the preparation of a potent .beta..sub.3 adrenergic receptor agonist. The instant invention also relates to processes for preparing the .beta..sub.3 adrenergic receptor agonist using the compounds of Formula II and Formula III.

Process and intermediates for a .beta..sub.3 -adrenergic receptor agonist

A method for preparing hydroxamic acid derivatives which are useful as analgesic, antiinflammatory, or neuroprotective agents.

Process for pyrrolidinyl hydroxamic acid compounds

(C.sub.1 -C.sub.3)Alkyl-4,6,7,8,9,9a-hexahydro-2H,3H-pyrido[1,2-a]pyrazin-1-one-7-c arboxylate esters, important precursors to certain bis-aza-bicyclic anxiolytics, can be prepared from di(C.sub.1 -C.sub.3)alkyl cis-piperidine-2,5-dicarboxylate starting material by a new process via a new class of intermediates, di(C.sub.1 -C.sub.3)alkyl cis-N-(2-(phthalimido)ethyl)piperidine-2,5-dicarboxylates. In the process, the starting material is reacted with either 2-(phthalimido)ethyl triflate or 2-(phthalimido)acetaldehyde to form the new intermediate, which can then be cyclized to the aforementioned precursor.

Process and intermediate for certain bis-aza-bicyclic anxiolytic agents

(C.sub.1 -C.sub.3)Alkyl-4,6,7,8,9,9a-hexahydro-2H,3H-pyrido-[1,2-a]pyrazin-1-one-7- carboxylate esters, important precursors to certain bis-aza-bicyclic anxiolytics, can be prepared from di(C.sub.1 -C.sub.3)alkyl cis-piperidine-2,5-dicarboxylate starting material by a new process via a new class of intermediates, di(C.sub.1 -C.sub.3)alkyl cis-N-(2-(phthalimido)ethyl)piperidine-2,5-dicarboxylates. In the process, the starting material is reacted with either 2-(phthalimido)ethyl triflate or 2-(phthalimido)acetaldehyde to form the new intermediate, which can then be cyclized to the aforementioned precursor.

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Old Lyme, CT, United States of America

Brian C Vanderplas