George Wu

6372909, Apr 16, 2002

Nov 18, 1999

09/442512

Charles F. Bernard - Agoura Hills CA
Michael Casey - Dublin, IE
Frank Xing Chen - Plainsboro NJ
Denise C. Grogan - Cork, IE
Marc Poirier - Edison NJ
Robert P. Williams - Enniskerry, IE
George G. Wu - Basking Ridge NJ

Schering Corporation - Kenilworth NJ

C07F 980

546 93, 546 2, 546 3, 546316

Disclosed is a process for preparing a compound having the formula: wherein R, R , R , R , and R are independently selected from the group consisting of H, Br, Cl, F, alkyl, or alkoxy, by (A) reacting a compound having the formula âwherein R , R , R , and R are independently selected from the group consisting of H, halo, alkyl, or alkoxy, and R is aryl or heteroaryl, with a dehydrating agent to produce an imine having the formula: (B) hydrolyzing the imine produced in step (A) to produce the compound having formula (I). Also disclosed are novel intermediates having the formula: âwherein R , R , R , R , and R are independently selected from the group consisting of H, halo, alkyl, or alkoxy, and R is aryl or heteroaryl. Also disclosed is a process for preparing a compound having the formula: âcomprising: reacting a compound having the formula: âwith NH R in the presence of a palladium catalyst, carbon monoxide, a base, and an ether selected from the group consisting of: CH OCH CH OCH ; CH OCH CH OCH CH OCH ; and CH OCH CH OCH CH OCH CH OCH , wherein X is H, Br, Cl, or F, and R is aryl or heteroaryl. The compounds made by these processes are useful intermediates for preparing compounds that are antihistamines or inhibitors of farnesyl protein transferase.

6492519, Dec 10, 2002

Apr 17, 2001

09/836605

Marc Poirier - Edison NJ
George G. Wu - Basking Ridge NJ

Schering Corporation - Kenilworth NJ

C07D22106

546 93, 546323, 546334

A process is provided for preparing a compound having the formula comprising: (a) reacting a compound having the formula with an isocyanate having the formula R NCO to produce a compound having the formula (b) optionally hydrolyzing the compound of formula (III) to form an amide having the formula (c) reacting the compound of formula (III) or the amide of formula (IV) with a compound having the formula in the presence of a strong base to produce a compound having the formula and (d) cyclizing the compound of formula (VI) to obtain the compound of formula (I), wherein R is H or Cl; M is selected from the group consisting of Li, Na, K, MgX, ZnR , and Al(R ) ; R is alkyl; X is halo; R is selected from the group consisting of alkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, and heterocycloalkylalkyl; and L is a leaving group.

6495689, Dec 17, 2002

Jun 21, 2001

09/886845

Charles F. Bernard - Agoura Hills CA
Michael Casey - Dublin, IE
Frank Xing Chen - Plainsboro NJ
Denise C. Grogan - Cork, IE
Marc Poirier - Edison NJ
Robert P. Williams - Enniskerry, IE
George G. Wu - Basking Ridge NJ

Schering Corporation - Kenliworth NJ

C07D22116

546 93

Disclosed is a process for preparing a compound having the formula: wherein R, R , R , R , and R are independently selected from the group consisting of H, Br, Cl, F, alkyl, or alkoxy.

6750347, Jun 15, 2004

Jun 18, 2002

10/174145

Marc Poirier - Edison NJ
George G. Wu - Basking Ridge NJ

Schering-Corporation - Kenilworth NJ

C07D22122

546 93, 546 79

A process is provided for preparing a compound having the formula wherein R is H or Cl. Also provided is a process for preparing a compound having the formula.

20140058116, Feb 27, 2014

May 2, 2012

14/114251

Ji Xie - Edison NJ, US
George Wu - Basking Ridge NJ, US
Joseph Lamberson - Jersey City NJ, US
Marc Poirier - Stewartsville NJ, US
Frank Chen - Plainsboro NJ, US

C07D 209/52

548515

The present invention relates to synthetic processes useful in the preparation of compounds of Formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease and have application in the treatment of conditions caused by HCV. In particular, the present invention relates to novel oxidation processes useful for preparing compounds of Formula (I) and related compounds, including pharmaceutically acceptable salts, hydrates and solvates thereof, and including stereoisomers thereof.

63070480, Oct 23, 2001

Nov 18, 1999

9/442511

Shen-Chun Kuo - Union NJ
Charles F. Bernard - Agoura Hills CA
Frank Xing Chen - Plainsboro NJ
Donald Hou - Verona NJ
George G. Wu - Basking Ridge NJ

Schering Corporation - Kenilworth NJ

C07D40102

546 93

Disclosed is a process for preparing a compound of the formula: ##STR1## wherein X. sup. 1, X. sup. 2, X. sup. 3, X. sup. 4, and X. sup. 5 are independently selected from the group consisting of H, halo, alkyl, alkoxy, aryl, and aryloxy, and R is a protecting group, in which a compound having the formula ##STR2## wherein X. sup. 1, X. sup. 2, X. sup. 3, X. sup. 4, and X. sup. 5 are as defined above, is treated with the following, in any sequence: (a) a non-nucleophilic strong base; (b) a chiral amino alcohol; and (c) a compound having the formula ##STR3## wherein L is a leaving group and R is as defined above. The compounds made by this process are useful intermediates for preparing compounds that are inhibitors of farnesyl protein transferase.