Merck + Co., Inc.

Gilead Sciences, Inc.

Norihiro Ikemoto

Nolan Griggs

Spencer Dreher

John Enquist, Jr

Christopher Hale

Scott E Lazerwith

Gerald F Bills

Mark E Scott

Michel M Chartrain

Anthony O King

Daniel Richard Sidler

Katie Ann Keaton

Colleen S Taylor

Henry Morrison

Andrew W Waltman

Luke Humphreys

J Michael Williams

Anna Chiu

Christopher Roberge

Jinchu Liu

Michael Geier

C Scott Shultz

Sean Liew

Vimal Varghese

Matt Kraft

Michel Leeman

Zhihui Peng

Kate Schrier

Jonathan Trinidad

Jochem Van Herpt

Michael M Chartrain

John Enquist

Methods of making compounds of Formula I are disclosed: 

Synthesis of polycyclic-carbamoylpyridone compounds

The present disclosure provides solid forms, including a salt or co-crystal, of Compound I: which exhibits Acetyl-CoA carboxylase ('ACC') inhibitory activity and may be useful in treating ACC mediated diseases. Also provided herein are processes or steps for the preparation of a Compound I and intermediates useful for the processes or steps described herein.

Processes for preparing ACC inhibitors and solid forms thereof

This invention relates to a process for preparing optically active &#x3b1;-amino acid substrates which are used to make potent lethal factor (LF) inhibitors for the treatment of anthrax. This invention further relates to a process for synthesis of potent LF-inhibitors for the treatment of anthrax. Specifically, the invention concerns a novel, high-yielding and highly enantioselective asymmetric hydrogenation reaction of a tetrasubstituted ene-sulfonamide acid or ester.

Process for making N-sulfonated-amino acid derivatives

The present invention is concerned with a process for the preparation of trifluorophenylacetic acids using a Grignard reagent and an allylating agent, such as allyl bromide.

Process for the synthesis of trifluorophenylacetic acids

A process for preparing &ggr;-hydroxy-4-&lsqb;&lsqb;2-oxazolyl&rsqb;alkyl&rsqb;-&agr;-&lsqb;(cyclo)alkyl- or aryl- or heteroaryl-substituted methyl&rsqb;-2-&lsqb;&lsqb;(un)substituted alkyl&rsqb;aminocarbonyl&rsqb;-1-piperazinepentanamides is disclosed. The piperazinepentanamides are useful as HIV protease inhibitors. A process for making a 4-&lsqb;&lsqb;2-oxazolyl&rsqb;alkyl&rsqb;-2-&lsqb;&lsqb;(un)substituted alkyl&rsqb;aminocarbonyl&rsqb;piperazine by treating a ketoamide precursor with fuming sulfuric acid in the presence of polyphosphoric acid is also disclosed. In addition, a process for enhancing the optical purity of 4-&lsqb;&lsqb;2-oxazolyl&rsqb;alkyl&rsqb;-2-&lsqb;&lsqb;(un)substituted alkyl&rsqb;aminocarbonyl&rsqb;-piperazines via the formation 2-naphthalenesulfonic acid crystal salts thereof is disclosed, as well as a method for purifying 2-naphthalenesulfonic acid.

Process for preparing piperazinepentaneamide HIV protease inhibitors

This invention relates to crystalline pharmaceutically acceptable salts of an alpha 1a adrenergic receptor antagonist, Compound A, which are useful in the treatment of benign prostatic hyperplasia. Pharmaceutical compositions employing the crystalline salts, and processes for making and using the crystalline salts and pharmaceutical compositions of Compound A are also disclosed. This invention further relates to a process for obtaining enantiomerically pure intermediate useful for the synthesis of end product alpha 1a adrenergic receptor antagonists. The end product compounds are useful for the treatment of benign prostatic hyperplasia and for relaxing lower urinary tract tissue. The invention also relates to a process for preparing a class of dihydropyrimidinone compounds of which Compound A is a member, wherein the process involves deprotonating a dihydropyrimidinone compound and then coupling the deprotonated derivative with a primary amine.

Enzymatic process of making alpha 1a adrenergic receptor antagonists using protease

A process for preparing cis-(1S,2R)-indanediol is disclosed. The process comprises (A) fermenting a culture medium containing a yeast strain selected from the group consisting of,MY 1506 (ATCC 74440) and mutants thereof and 1,2-indanedione to form cis-(1S,2R)-indanediol; and (B) recovering cis-(1S,2R)-indanediol from the culture medium. A process for preparing (1S)-amino-(2R)-indanol from the recovered cis-(1S,2R)-indanediol via the Ritter reaction is also disclosed.

Process for the preparation cis-(1S,2R)-indanediol by direduction of 1,2-indanedione using trichosporon cutaneum

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Edison, NJ, United States of America

Norihiro Ikemoto