G.d. Searle & Company

Pharmacia Corporation

Pharmacia Corporation (of Pfizer, Inc.)

Chin Liu

John S Ng

Bernhard Erb

Yuen-Lung L Sing

Leo J Letendre

Joseph J Wieczorek

Mark John Pozzo

Edward E Yonan

Jon P Lawson

Dennis K Anderson

Sastry A Kunda

Ping T Wang

Julio A Baez

Gennaro Mucciariello

Fortunato Vanzanella

Richard A Mueller

Daniel P Getman

Gary A DeCrescenzo

Michael L Vazquez

Richard M Weier

Robert M Heintz

Deborah E Bertenshaw

Scott A Laneman

Claire A Przybyla

Thomas R Kowar

John J Freskos

Suhong Zhang

James R Behling

Arthur L Campbell

Multiple novel keto-substituted intermediates are provided for the synthesis of epoxymexrenone, useful as an Aldosterone Receptor Antagonist.

Keto-substituted steroid compounds

Intermediates in the preparation of 9,11-epoxy steroids are disclosed. Particularly, disclosed are 11,12-epoxy steroid, 4,5-9,11-diepoxy steroid and 12-keto steroid intermediates.

Processes for preparation of 9,11-epoxy steroids and intermediates useful therein

Multiple novel reaction schemes, novel process steps and novel intermediates are provided for the synthesis of epoxymexrenone and other compounds of Formula Iwherein:

Process for preparation of 9, 11-epoxy steroids and intermediates useful therein

Multiple novel reaction schemes, novel process steps and novel intermediates are provided for the synthesis of epoxymexrenone and other compounds of Formula Iwherein: &#x2014;A&#x2014;A&#x2014;, &#x2014;B&#x2014;B&#x2014;, R, R, Rand Rare as defined in the specification.

Processes for the preparation of 4,5-dihydro-5,7-lactone steroid compounds are provided.

Processes for preparation of 9, 11-epoxy steroids and intermediates useful therein

Process for preparation of 9,11-epoxy steroids and intermediates useful therein

5&bgr;-cyano-substituted steroid compounds

A process for the formation of an epoxy compound comprising contacting a substrate compound having an olefinic double bond with a peroxide compound in the presence of a peroxide activator, said peroxide activator corresponding to the formula:

Multiple novel reaction schemes, novel process steps and novel intermediates are provided for the synthesis of epoxymexrenone, useful as a diuretic, and other compounds of Formula I

Keto-Substituted Steroid Compounds

Multiple reaction schemes, process steps and intermediates are provided for the synthesis of epoxymexrenone, useful as a diuretic, and other compounds of Formula I

In a method of preparing an aminoepoxide wherein a protected aminoaldehyde is reacted with a halomethyl organometallic reagent in an appropriate solvent at a temperature above -80.degree. C., wherein said halomethyl organometallic reagent is formed by reaction between an organometallic reagent and a dihalomethane, the improvement comprising flowing said protected aminoaldehyde into a mixing zone maintained at a temperature below 0.degree. C., also flowing said halomethyl organometallic reagent in said mixing zone for contacting in said mixing zone with said protected aminoaldehyde and also withdrawing from said mixing zone reaction products of said protected aminoaldehyde and said halomethyl organometallic reagent.

Epoxide formation by continuous in-situ synthesis process

Multiple reaction schemes, process steps and intermediates are provided for the synthesis of epoxymexrenone, useful as a diuretic, and other 9,11-epoxy-steroids.

Processes for preparation of 9,11-epoxy steroids and intermediates

A synthesis is described for intermediates which are readily amenable to the large scale preparation of hydroxyethylurea-based chiral HIV protease inhibitors. The method includes forming a diastereoselective epoxide or cyanohydrin from a chiral alpha amino aldehyde.

Growing community of inventors

Vernon Hills, IL, United States of America

Chin Liu