David H. B. Ripin - Westbrook CT Brian C. Vanderplas - Old Lyme CT Takushi Kaneko - Guilford CT William T. McMillen - Fisher IN Robert W. McLaughlin - Groton CT
Assignee:
Pfizer Inc. - New York NY
International Classification:
C07H 100
US Classification:
536 74, 536 185
Abstract:
The invention relates to a method of preparing a macrolide antibiotic of the formula wherein R , R , R , R , R are defined above. These antibiotics are useful as antibacterial and antiprotozoal agents in mammals, including man, as well as in fish and birds. The invention also includes novel compounds made by the preparation of the macrolide antibiotic.
Preparation Of 3-Azabicyclo [3.1.0] Hexane Derivatives
Stanton Furst McHardy - Coventry RI, US John Anthony Ragan - Gales Ferry CT, US Derek Lawrence Tickner - Waterford CT, US Brian Clement Vanderplas - Old Lyme CT, US Jotham Wadsworth Coe - Niantic CT, US
International Classification:
A61K 31/403 C07D 209/52
US Classification:
514412, 548515
Abstract:
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.
Process For Pyrrolidinyl Hydroxamic Acid Compounds
Keith M. DeVries - Chester CT Jeffrey W. Raggon - Uncasville CT Ravi M. Shanker - Groton CT Frank J. Urban - Waterford CT Brian C. Vanderplas - Old Lyme CT
Assignee:
Pfizer Inc. - New York NY
International Classification:
C07F 702 C07D40512 C07D40312
US Classification:
546 14
Abstract:
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 Intermediate For Certain Bis-Aza-Bicyclic Anxiolytic Agents
Dennis M. Godek - Glastonbury CT Charles W. Murtiashaw - North Stonington CT Frank J. Urban - Waterford CT Brian C. Vanderplas - Niantic CT
Assignee:
Pfizer Inc. - New York NY
International Classification:
C07D47104 C07D22700
US Classification:
544349
Abstract:
(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
Dennis M. Godek - Glastonbury CT Charles W. Murtiashaw - North Stonington CT Frank J. Urban - Waterford CT Brian C. Vanderplas - Niantic CT
Assignee:
Pfizer Inc. - New York NY
International Classification:
C07D227093 C07D47104
US Classification:
546272
Abstract:
(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.
Process And Intermediates For A .Beta..sub.3 -Adrenergic Receptor Agonist
Keith M. DeVries - Chester CT Jeffrey W. Raggon - Uncasville CT Ravi M. Shanker - Groton CT Frank J. Urban - Waterford CT Brian C. Vanderplas - Old Lyme CT
Assignee:
Pfizer Inc. - New York NY
International Classification:
C07F 702 C07D40502 C07D21174 C07D21353
US Classification:
546 14
Abstract:
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.
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