Schering Corporation

Merck Sharp + Dohme Corp.

Opko Health, Inc.

Xiaoyong Fu

Timothy L McAllister

Tiruvettipuram K Thiruvengadam

Jianguo Yin

Chou-Hong Tann

Shuyi Zhang

Agnes S Kim-Meade

Wenxue Wu

John S Chiu

Cesar Colon

Jason L Winters

Anantha R Sudhakar

Doris P Schumacher

Kelvin Yong

Gerald Werne

George G Wu

Frank Xing Chen

Marc Poirier

David R Andrews

Dinesh Gala

Ilia A Zavialov

Tao Wang

Hongbiao Liao

Robert Kevin Orr

Gary M Lee

Jing Liao

Hong-Chang Lee

Ji Xie

Junning Lee

Ingrid Mergelsberg

Jian Cui

Fucheng Zhang

David J Tsai

Martin Lawrence Schwartz

Victoria M Sprague

David J S Tsai

Liansheng Zeng

Louis Peter Castellanos

Yuyin Chen

Donal Maloney

Chou-Hang Tann

Arthur G Taveras

Michael P Dwyer

David J Blythin

Younong Yu

Ho-Jane Shue

Rongze Kuang

Xiao Chen

Kevin Joseph Klopfer

Scott Trzaska

David Jieh-Shyh Tsai

Xiaoming Chen

Michael R Reeder

Daw-Iong Albert Kwok

Kenneth Stanley Matthews

Mengwei Hu

Mathew Thomas Maust

Vincenzo Liotta

T K Thiruvengadam

Frank Bruno Guenter

Thiruvettipuram K Thiruvengadam

Timothy D Cutarelli

Chee-Wah Tang

Zaher Shabani

Kelvin H Yong

Yianguo Yin

Timothy L Macallister

Thiruvengadam K Thiruvettipuram

Timothy Mcallister

This application discloses a novel process to synthesize 8-[{1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds, which may be used, for example, as NK-1 inhibitor compounds in pharmaceutical preparations, intermediates useful in said process, and processes for preparing said intermediates; also disclosed is a process for removal of metals from N-heterocyclic carbine metal complexes.

Process and intermediates for the synthesis of 8-[{1-(3,5-bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds

This application discloses a novel process for the preparation of 1,2-substituted 3,4-dioxo-1-cyclobutene compounds, which have utility, for example, in the treatment of CXC chemokine-mediated diseases, and intermediates useful in the synthesis thereof.

Process and intermediates for the synthesis of 1,2-substituted 3,4-dioxo-1-cyclobutene compounds

A process is provided for preparing azetidinones useful as intermediates in the synthesis of penems and as hypocholesterolemic agents, comprising reacting a &#x3b2;-(substituted-amino)amide, a &#x3b2;-(substituted-amino)acid ester, or a &#x3b2;-(substituted-amino)thiolcarbonic acid ester with a silylating agent and a cyclizing agent selected from the group consisting of alkali metal carboxylates, quaternary ammonium carboxylates, quaternary ammonium hydroxides, quaternary ammonium alkoxides, quaternary ammonium aryloxides and hydrates thereof, or the reaction product of: (i) at least one quaternary ammonium halide and at least one alkali metal carboxylate; or (ii) at least one quaternary ammonium chloride, quaternary ammonium bromide, or quaternary ammonium iodide and at least one alkali metal fluoride, wherein a quaternary ammonium moiety of the cyclizing agent is unsubstituted or substituted by one to four groups independently selected from the group consisting of alkyl, arylalkyl and arylalkyl-alkyl.

Process for the synthesis of azetidinones

This application discloses a novel process for the preparation of phosphonate esters useful as intermediates in the preparation of himbacine analogs, themselves useful as thrombin receptor antagonists. The chemistry taught herein can be exemplified by the following scheme: wherein Ris selected from alkyl, aryl heteroaryl and arylalkyl groups having 1 to 10 carbon atoms, and Ris selected independently for each occurrence from alkyl, aryl heteroaryl and arylalkyl groups having 1 to 10 carbon atoms and hydrogen, Xis Cl, Br, or I; Xis selected from Cl and Br; and PdLis a supported palladium metal catalyst or a soluble heterogeneous palladium catalyst. The L-derivatizing reagent is a moiety which converts the alcohol functional group of compound 137D to any leaving group which can be displaced by a triorgano-phosphite phosphonating agent.

Synthesis of diethyl{[5-(3-fluorophenyl)-pyridine-2yl]methyl}phosphonate

The present invention relates to four distinct crystalline polymorphs of a monohydrate of Compound A having the following chemical structure:  These four polymorphic forms, herein referred to as Forms I, II, III and IV are active as a CXC-chemokine receptor ligands. The invention is further directed to formulations, methods of treatment, and processes of synthesis of these polymorphic forms.

Crystalline polymorphs of a CXC-chemokine receptor ligand

This application discloses a novel process to synthesize 2-(Quinolin-5yo)-4,5-Disubstituted-Azole derivatives, which may be used, for example, as PDE IV inhibitor compounds in pharmaceutical preparations.

Process and intermediates for the synthesis of 2-(quinolin-5-yl)-4,5 disubstituted-azole derivatives

Disclosed are maleate, tosylate, fumarate, and oxalate salts of the compound 5-(1(S)-Amino-2-Hydroxyethyl)-N-[(2,4-Difluorophenyl)-Methyl]-2-[8-Methoxy-2-(Trifluoromethyl)-5-Quinoline]-4-Oxazolecarboxamide, represented by Formula I, and methods of preparing the same.

Maleate, tosylate, fumarate and oxalate salts of 5-(1-(S)-amino-2-hydroxyethyl)-N-[(2,4-difluorophenyl)-methy]-2-[8-methoxy-2-(triflouromethy)-5-quinoline]-4-oxazolecarboxamide and preparation process therefore

Disclosed is a process for making the compound of formula I: using the compounds of formulas II, Q, and XI or XII: wherein A is selected from the group consisting of Br, Cl and I (with Br being preferred); and R represents (C-C)alkyl. Also disclosed are intermediate compounds that are made in the disclosed process.

Synthesis of 2-Hydroxy-N,N-dimethyl-3-[[2-[[1(R)-(5-methyl-2-furanyl)propyl]amino]-3,4-dioxo-1-cyclobuten-1-yl]amino]benzamide

In an illustrative embodiment, the present invention describes the synthesis of the following compound and similar compounds, in high stereochemical purity by a novel stereoselective alkylation process: 

Stereoselective alkylation of chiral 2-methyl-4-protected piperazines

The present invention relates to an improved process for preparing himbacine analogs. The compounds are useful as thrombin receptor antagonists. The improved process may allow for at least one of easier purification by crystallization, easier scalability, and improved process yield on the desired enantiomer. An example of a step in the synthesis of such a himbacine analog is as follows: 

Synthesis of himbacine analogs

Synthesis of 2-hydroxy-n,n-dimethyl-3-[[2-[[1(r)-(5-methyl-2-furanyl)propyl]amino]-3,4-dioxo-1-cyclobuten-1-yl]amino]benzamide

Disclosed is a process for making the compound of formula I: using the compounds of formulas II, Q, and XI or XII: wherein A is selected from the group consisting of Br, Cl and I (with Br being preferred); and R represents (C&#x2013;C)alkyl. Also disclosed are intermediate compounds that are made in the disclosed process.

Synthesis of 2-hydroxy-N,N-dimethyl-3-[ [2-[1 (R)-(5-methyl-2-furanyl)propyl]amino]-3,4-dioxo-1-cyclobuten-1-yl]aminobenzamide

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Edison, NJ, United States of America

Xiaoyong Fu