Schering Corporation

Merck Sharp + Dohme Corp.

University of Southern California

Ilia A Zavialov

Hoa N Nguyen

Anantha R Sudhakar

Tiruvettipuram K Thiruvengadam

Cecilia A Orr

George G Wu

Frank Xing Chen

Marc Poirier

Tao Wang

Xiaojing Yang

Jing Liao

Ji Xie

Mingsheng Huang

Ngiap Kie Lim

Jian Cui

Vijay Sabesan

Nicos A Petasis

Xiaoyong Fu

Jianguo Yin

Vilas Hareshwar Dahanukar

Daw-long Albert Kwok

Ingyu Jeon

Fucheng Zhang

Kelvin Yong

Vilas H Dahanukar

Vilas A Dahanukar

Nobuyoshi Yasuda

Wenxue Wu

Craig D Boyle

William W Leong

Hongmei Li

Peter Emmanuel Maligres

Dinesh Gala

Minzhang Chen

Kevin Joseph Klopfer

Artis Klapars

Doris P Schumacher

Jeonghan Park

George S Wong

Jeffrey Manning Eckert

Michael D Green

Hong-Chang Lee

Loc Thanh Tran

Yonggang Chen

Ian Mangion

Juergen Weber

Feng Liang

Bosco D'Sa

Daw-Iong Albert Kwok

Xiongwei Shi

Man Zhu

Tetsuo Iwama

Cheng-yi Chen

Yi Liu

Brian Lucas

Albert W Buchholz, Jr

Jeffrey M Skell

Funcheng Zhang

Zubin D Patel

Shannon Zhao

Cecelia Proietti

Thiruvettipuram K Thiruvengadam

Kelvin H Yong

Cecilia Proietti

Xiongwei Shih

The present invention is directed to a process for preparing Tetracyclic Heterocycle Compounds of formula (I): which are useful as HCV NS5A inhibitors. The present invention is also directed to compounds that are useful as synthetic intermediates for making the compounds of formula (I). 

Process for preparing tetracyclic heterocycle compounds

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

This application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center. The chemistry taught herein can be exemplified by the following: 

Exo- and diastereo- selective synthesis of himbacine analogs

Exo- and diastereo-selective syntheses of himbacine analogs

A process for preparing xanthine phosphodiesterase V inhibitors, and compounds utilized in said process. The process includes a five-step methodology for efficient synthesis of Compound 5 without intermediate purifications or separations, a dihalogenation step to synthesize Compound 7, and a coupling reaction to produce Compound 9.   

Process for preparing xanthine phosphodiesterase V inhibitors and precursors thereof

The present invention is directed to the synthesis of 4-[4-[(R)-[1-[cyclopropylsulfonyl)-4-piperidinyl](3-fluorophenyl)methyl]-3(S)-methyl-1-piperazinyl]-1-[(4,6-dimethyl-5-pyrimidinyl)carbonyl]-4-methylpiperidine], and intermediates therefor from readily available starting materials by a novel route.

Synthesis of CCR5 receptor antagonists

Exo- and diastereo- selective syntheses of himbacine analogs

Synthetic methods provide for the simple, efficient preparation of amino polyols and derivatives. The methods include a three-component reaction of a carbohydrates with organoboron compounds and primary or secondary amine derivatives. The resulting amino polyols can be transformed into amino sugars. In one implementation, the amine moiety is protected, and an alkenyl, aryl or heteroaryl moiety is cleaved to form the amino sugar. Amino polyols and amino sugars prepared according to the methods are also described.

Amino polyols and amino sugars

In one embodiment, the present application relates to a process of making a compound of formula I: and to certain intermediate compounds that are made within the process of making the compound of formula I.

Process and intermediates for the preparation of (1R,2S,5S)-3-azabicyclo[3,1,0]hexane-2-carboxamide, N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3-[(2S)-2-[[[1,1-dimethylethyl]amino]carbonylamino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl

Crystalline polymorphs of 1-ethyl-3,7-dihydro-8-[(1R,2R) -(hydroxycyclopentyl)amino]-3-(2-hydroxyethyl)-7-[(3-bromo-4-methoxyphenyl)methyl]-1H-Purine-2,6-dione in Form 1 and Form 2, which exhibit x-ray powder diffraction profiles substantially the same as those shown in FIGS.and, respectively, and which exhibit differential scanning calorimtery profiles substantially the same as those shown in FIGS.and, respectively, and are represented by the formula:  Pharmaceutical compositions comprising the polymorph Form 1 or 2 of Compound 13 and at least one excipient or carrier, and methods of using the polymorph Form 1 or 2 of Compound 13 to treat a variety of physiological disorders, such as erectile dysfunction.

Xanthine phosphodiesterase V inhibitor polymorphs

A process for preparing xanthine phosphodiesterase V inhibitors, and compounds utilized in said process. The process includes a five-step methodology for efficient synthesis of Compound 5 without intermediate purifications or separations, a dihalogenation step to synthesize Compound 7, and a coupling reaction to produce Compound 9 

In one embodiment, the present invention describes the synthesis of a compound of formulaand intermediates therefor.

Process for synthesis of D1 receptor antagonists

Amines and amino acids are prepared by reacting an amine, a carbonyl derivative, and an organoboron compound under mild conditions.

Method for the synthesis of amines and amino acids with organoboron derivatives

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Princeton, NJ, United States of America

Ilia A Zavialov