Title:
PROCESS FOR MAKING CHIRAL 1,4-DISUBSTITUTED PIPERAZINES
Document Type and Number:
WIPO Patent Application WO2003078420
Kind Code:
A3
Abstract:
A process for a stereoselective preparation of novel chiral nitrogen mustard derivatives useful in synthesizing optically active 1,4-disubstituted piperazines of formula (I) wherein R, Ar, and Q are defined as set forth herein, and intermediate compounds therefor. The 1,4-disubstituted piperazines act as 5HT1A receptor binding agents useful in the treatment of Central Nervous System (CNS) disorders.
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Inventors:
JIRKOVSKY IVO (US)
ZELDIS JOSEPH (US)
FEIGELSON GREGG BRIAN (US)
ZELDIS JOSEPH (US)
FEIGELSON GREGG BRIAN (US)
Application Number:
PCT/US2003/007176
Publication Date:
March 11, 2004
Filing Date:
March 10, 2003
Export Citation:
Assignee:
WYETH CORP (US)
JIRKOVSKY IVO (US)
ZELDIS JOSEPH (US)
FEIGELSON GREGG BRIAN (US)
JIRKOVSKY IVO (US)
ZELDIS JOSEPH (US)
FEIGELSON GREGG BRIAN (US)
International Classes:
C07B53/00; C07C229/12; C07D295/08; C07D213/75; C07D295/10; C07D319/18; C07D401/00; C07D405/12; C07D487/10; (IPC1-7): C07D319/18; C07C229/12
Foreign References:
| DE960203C | 1957-03-21 |
Other References:
DATABASE CROSSFIRE BEILSTEIN [online] Beilstein Institut zur Förderung der Chemischen Wissenschaften, Frankfurt am Main, DE; XP002252515, Database accession no. 3915193
DATABASE CROSSFIRE BEILSTEIN [online] Beilstein Institut zur Förderung der Chemischen Wissenschaften, Frankfurt am Main, DE; XP002252516, Database accession no. 1512459
S. J. STACHEL ET AL.: "A Chiral C3 Triisopropylamine and its Silatrane Derivatives", TETRAHEDON LETTERS, vol. 40, 1999, pages 5811 - 5812, XP002252511
J. M. C. GOLEC ET AL.: "Structure-based design of non-peptidic pyridone aldehydes as inhibitors of interleukin-1.beta. converting enzyme", BIORG. MED. CHEM. LETT., vol. 7, no. 17, 1997, pages 2181 - 2186, XP002252512
D. MULLER ET AL.: "Building Units for N-Backbone Cyclic Peptides. 3. Synthesis of Protected N.alpha.-(.omega.-Aminoalkyl)amino Acids and N.alpha.-(.omega.-Carboxyalkyl)amino Acids", J. ORG. CHEM., vol. 62, no. 2, 1997, pages 411 - 416, XP002252513
G. M. TAYLOR ET AL.: "On The Ritter Reaction of Cyclic Hydroxyamines: Synthesis of Conformationally-Restricted Reduced Amide Dipeptide Isosteres", TETRAHEDRON LETTERS, vol. 37, no. 8, 1996, pages 1297 - 1300, XP002252514
DATABASE CROSSFIRE BEILSTEIN [online] Beilstein Institut zur Förderung der Chemischen Wissenschaften, Frankfurt am Main, DE; XP002252516, Database accession no. 1512459
S. J. STACHEL ET AL.: "A Chiral C3 Triisopropylamine and its Silatrane Derivatives", TETRAHEDON LETTERS, vol. 40, 1999, pages 5811 - 5812, XP002252511
J. M. C. GOLEC ET AL.: "Structure-based design of non-peptidic pyridone aldehydes as inhibitors of interleukin-1.beta. converting enzyme", BIORG. MED. CHEM. LETT., vol. 7, no. 17, 1997, pages 2181 - 2186, XP002252512
D. MULLER ET AL.: "Building Units for N-Backbone Cyclic Peptides. 3. Synthesis of Protected N.alpha.-(.omega.-Aminoalkyl)amino Acids and N.alpha.-(.omega.-Carboxyalkyl)amino Acids", J. ORG. CHEM., vol. 62, no. 2, 1997, pages 411 - 416, XP002252513
G. M. TAYLOR ET AL.: "On The Ritter Reaction of Cyclic Hydroxyamines: Synthesis of Conformationally-Restricted Reduced Amide Dipeptide Isosteres", TETRAHEDRON LETTERS, vol. 37, no. 8, 1996, pages 1297 - 1300, XP002252514
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