Wyeth

Pfizer Corporation

Wyeth Holdings Corporation

Genaera Corporation

Ohr Pharmaceutical Inc.

Ronald Stanley Michalak

Panolil C Raveendranath

Christoph Martin Dehnhardt

Mousumi Ghosh

Mahmut Levent

Michael William Winkley

Charles Guinosso

Ara R Boyajian

Michel Cantin

Alan Stockton

Frederick J Vyverberg

William Alvin Kinney

Sreenivasulu Megati

Joseph Zeldis

Xuehai Zhang

David Michael Blum

Jianxin Ren

Jean Louise Helom

Sylvain Daigneault

Michel Bernatchez

Timothy John Doyle

Charles Chao Wu

Yangzhong Wu

Mel Jennings

The present invention provides a compound of formula 1: wherein Ris CF, Ris H' Ris H.

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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

The present invention provides method for making a compound of formula 1: comprising the steps of reacting compounds of formulas 2 and 3: to produce a compound of formula 4: wherein R, R, R, Rand Rare defined as described herein. The compound of formula 4 is then converted to the compound of formula 1. The invention further comprises compounds of formulas 3 and 4 and methods for making compounds of formulas 3 and 4.

An efficient method for the synthesis of aminosterol compounds such as squalamine and compound 1436 is described. A method of the invention provides for regioselective sulfonation of a fused ring system. The fused ring system base can be, for example, a steroid ring base. The aminosterol compounds are effective as, among others, antibiotics, antiangiogenic agents and NHE3 inhibitors.

Regioselective and stereoselective oxidation of fused ring systems useful for the preparation of aminosterols

A process for the reductive alkylation at the C-3 position of an indole compound in which the indole is treated with an aldehyde in the presence of a Lewis acid and a silicon hydride reducing agent. The process is useful for alkylating the C-3 position of indoles that contain acid-sensitive substituents at the N-1 position.

Synthetic methodology for the reductive alkylation at the C-3 position of indoles

A process for making the compound of formula (I) wherein Ac represents acetate; X represents O or CH; Y represents C-Calkyl; and Z is selected from the group consisting of H, halogen, CN, CHO, CF, OCF, OH, C-Calkyl, C-Calkoxy, C-Cthioalkyl, NH, N(C-Calkyl), NH(C-Calkyl), NC(O)&#x2014;(CCalkyl), and NO. In his process, a compound of formula (II) is reacted with hydrazine to form a primary alkylamine, and then the primary alkylamine is reacted with acetic anhydride, to produce the compound of formula (I).

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

The present invention provides a process for the preparation of 6-amino-4-(3-chloro-4-fluoro-phenylamino)-7-ethoxy-quinoline-3-carbonitrile comprising the steps and products disclosed within this application.

Process for the synthesis of 6-amino-4-(3-chloro-4-fluoro-phenylamino)-7-ethoxy-quinoline-3-carbonitrile

A process for making a substituted indole compound, including the steps of: reacting the compounds in a non-protic polar solvent in the presence of a catalyst to form the intermediate compound wherein Ph and X are as defined herein; and then,heating this intermediate compound in the solvent in the presence of the catalyst to form the substituted indole compound The invention also includes compounds formed by this process.

The present invention provides processes for the preparation of arylalkylsulfonyl halides and heteroarylalkylsufonyl halides of Formula I: Ar&#x2014;R&#x2014;SO&#x2014;X, that are useful as intermediates in the preparation of pharmaceuticals.

Processes for the preparation of aryl- and heteroaryl-alkylsulfonyl halides

An efficient method for the synthesis of aminosterol compounds such as squalamine and compound 1436 is described. A method of the invention provides for regioselective oxidation and regioselective sulfonation of a fused ring system. The fused ring base can be, for example, a steroid ring base. The aminosterol compounds are effective as, for example, antibiotics, antiangiogenic agents and NHE3 inhibitors.

Growing community of inventors

Congers, NY, United States of America

Ronald Stanley Michalak