Wyeth

American Home Products Corporation

Wyeth Holdings Corporation

Ziarco Pharma Ltd.

Joseph Zeldis

Ivo L Jirkovsky

Gregg Brian Feigelson

Panolil C Raveendranath

Anita Wai-Yin Chan

Jianxin Ren

John R Potoski

Silvio Iera

Galina Vid

Ronald Stanley Michalak

Syed Muzafar Shah

Aranapakam Mudumbai Venkatesan

Jeremy Ian Levin

Tarek Suhayl Mansour

David Michael Blum

Arkadiy Zinoviy Rubezhov

Jean Schmid

Lalitha Krishnan

Jean Louise Helom

Mousumi Ghosh

Michael William Winkley

Michael Z Kagan

Leonard Alexander McDonald

Timothy John Doyle

Henry Strong

Gulnaz Khafizova

Ting-Zhong Wang

Antonia Nikitenko

Kenneth Alfred Martin Kremer

Fangming Kong

Huan-Qiu Li

Mellard Jennings

Zhixin Wen

Mel Jennings

Ronal Stanley Michalak

The present invention provides synthetic processes for the preparation of sulfonyl halides of Formula Ar&#x2014;(R)&#x2014;SO&#x2014;X and sulfonamides of Formula Ar&#x2014;(R)&#x2014;SO&#x2014;NRR, where the constituent variables are as defined herein, that are useful as intermediates in the preparation of pharmaceuticals.

Process for the synthesis of sulfonyl halides and sulfonamides from sulfonic acid salts

Processes for preparing amino alcohols or salts thereof and sulfonamide substituted alcohol compounds are provided. Desirably, the sulfonamide substituted alcohol compounds are heterocyclic sulfonamide trifluoroalkyl-substituted alcohol compounds or phenyl sulfonamide trifluoroalkyl-substituted alcohol compounds.

Methods for preparing sulfonamide substituted alcohols and intermediates thereof

The present invention relates to novel methods for the preparation of glutamic acid derivatives and intermediates thereof, and such compounds prepared by the novel methods.

Methods for preparing glutamic acid derivatives

A process for making a compound of the formula comprising dialkylating a benzodioxane aniline 

Preparation of N1-(2'-pyridyl)-1,2-propanediamine sulfamic acid and its use in the synthesis of biologically active piperazines

There is provided a process for the preparation of bicyclicheteroaryl carboxaldehydes having the structural Formula I where X and Y are defined in the specification  The bicyclic heteroaryl carboxaldehydes are useful as intermediates in the preparation of &#x3b2;-lactamase inhibitors.

Process for synthesizing beta-lactamase inhibitor intermediates

A process for a stereoselective preparation of novel chiral nitrogen mustard derivatives useful in synthesizing optically active 1,4-disubstituted piperazines of formula: wherein R, Ar, and Q are defined as set forth herein, and intermediate compounds therefor. The 1,4-disubstituted piperazines act as 5HT1A receptor binding agents useful in the treatment of Central Nervous System (CNS) disorders. The intermediate compounds of Formula II and IV as set forth herein are also included.

Process for making chiral 1,4-disubstituted piperazines

Processes for using a compound of formula III: to make compounds of formulae I and II: and processes for making the compound of formula III, where Rand J are as defined herein.

Method for preparing hydroxamic acids

A process for formation of N-aryl piperazines with chiral N'-1-[benzoyl(2-pyridyl)amino]-2-propane side-chains having the structure shown in formula below, and for making intermediate compounds therefor. In this process, chirality is introduced at the piperazine ring formation step and 2-aminopyridyl substitution is incorporated via displacement. The resulting N, N&#x2032; disubstituted piperazines act on the central nervous system at 5HT receptors.

Process for synthesizing N-aryl piperazines with chiral N'-1-[benzoyl(2-pyridyl)amino]-2-propane substitution

A process for a stereoselective preparation of novel chiral nitrogen mustard derivatives useful in synthesizing optically active 1,4-disubstituted piperazines of formula:wherein R, Ar, and Q are defined as set forth herein, and intermediate compounds therefor. The 1,4-disubstituted piperazines act as 5HT1A receptor binding agents useful in the treatment of Central Nervous System (CNS) disorders.

Preparation of N1-(2&prime;-pyridyl)-1,2-propanediamine sulfamic acid and its use in the synthesis of biologically active piperazines

Process for synthesizing N-aryl piperazines with chiral N&prime;-1-&lsqb;benzoyl(2-pyridyl)amino&rsqb;-2-propane substitution

This invention provides a pharmaceutically acceptable salt of 3&bgr;-hydroxy-5(10)-estrene-17-one 3-sulfate ester and a pharmaceutically acceptable salt of 3&agr;-hydroxy-5(10)-estrene-17-one 3-sulfate ester, which are useful as an estrogens.

Estrenes

The present invention provides compounds useful in the synthesis of biologically active compounds, and processes for their production, the compounds having the formula:

Aryloxy-alkyl-dialkylamines

The present invention provides compounds useful in the synthesis of biologically active compounds, and processes for their production, the compounds having the formula: ##STR1## wherein: R.sup.1 and R.sup.2 are, independently, selected from H; C.sub.1 -C.sub.12 alkyl or C.sub.1 -C.sub.6 perfluorinated alkyl; X represents a leaving group; A is O or S; m is an integer from 1 to 3, preferably 2; R.sup.3, R.sup.4, R.sup.5, and R.sup.6 are independently selected from H, halogen, --NO.sub.2, alkyl, alkoxy, C.sub.1 -C.sub.6 perfluorinated alkyl, OH or the C.sub.1 -C.sub.4 esters or alkyl ethers thereof, --CN, --O--R.sup.1, --O--Ar, --S--R.sup.1, --S--Ar, --SO--R.sup.1, --SO--Ar, --SO.sub.2 --R.sup.1, --SO.sub.2 --Ar, --CO--R.sup.1, --CO--Ar, --CO.sub.2 --R.sup.1, or --CO.sub.2 --Ar; and Y is selected from a) the moiety: ##STR2## wherein R.sub.7 and R.sub.8 are independently selected from the group of H, C.sub.1 -C.sub.6 alkyl, or phenyl; or b) an optionally substituted five-, six- or seven-membered saturated, unsaturated or partially unsaturated heterocycle or bicyclic heterocycle containing up to two heteroatoms selected from the group consisting of --O--, --NH--, --N(C.sub.1 C.sub.4 alkyl)--, --N.dbd., and --S(O).sub.n --.

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New City, NY, United States of America

Joseph Zeldis