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Literature References
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| 1. |
Vibha Oza, Susan Ashwell, Patrick Brassil, Jason Breed, Chun Deng, Jay Ezhuthachan,
Heather Haye, Candice Horn, James Janetka, Paul Lyne, Nicholas Newcombe, Ludo Otterbien,
Martin Pass, Jon Read, Sian Roswell, Mei Su, Dorin Toader, Dingwei Yu, Yan Yu, Anna Valentine,
Peter Webborn, Ann White, Sonya Zabludoff and Xiaolan Zheng
Discovery of a novel class of triazolones as Checkpoint Kinase inhibitors—Hit to lead exploration
Oza and co-workers at AstraZeneca disclose a novel class of aryl substituted triazoloquinolone Checkpoint Kinase-1 (Chk1) inhibitors. Such inhibitors were initially identified by high throughput screening methods and further optimized for potency and PK properties. Microwave irradiation of a mixture of BioBlocks QU3495 and ethyl-carbazate led to an intermediate bromo-triazoloquinolone which was further coupled with a variety of aryl-boronic acids via standard Suzuki coupling conditions.
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| 2. |
Fabrizio Giordanetto, Olle Karlsson, Jan Lindberg, Lars-Olof Larsson,
Anna Linusson, Emma Evertsson, David G. A. Morgane and Tord Inghardt
Discovery of cyclopentane- and cyclohexane-trans-1,3-diamines
as potent melanin-concentrating hormone receptor 1 antagonists
Giordanetto and co-workers at AstraZeneca present a series of cyclopentane- and cyclohexane-1,3-diamine-quinoline derivatives as novel and potent melanin-concentrating hormone receptor (MCH-R1) antagonists. The most active MCH-R1 antagonist in the report is dervived from BioBlocks QU3498 by palladium mediated coupling with Cbz-protected trans-cyclohexane-1,3-diamine followed by deprotection and finally reductive alkylation with thiophene-3-carbaldehyde.
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| 3. |
Dahui Zhou, Gary P. Stack, Jennifer Lo, Amedeo A. Failli, Deborah A. Evrard, Boyd L. Harrison,
Nicole T. Hatzenbuhler, Megan Tran, Susan Croce, Soo Yi, Jeannette Golembieski, Geoffrey A. Hornby, Margaret Lai, Qian Lin, Lee E. Schechter, Deborah L. Smith, Adam D. Shilling, Christine Huselton, Paul Mitchell, Chad E. Beyer and Terrance H. Andree
Synthesis, Potency, and in Vivo Evaluation of 2-Piperazin-1-ylquinoline Analogues as Dual Serotonin
Reuptake Inhibitors and Serotonin 5-HT1A Receptor Antagonists
Scientists at Wyeth Research report a series of 2-piperazinyl- and 2-(1,4)-diazepane- quinoline derivatives as dual-acting serotonin (5-HT) reuptake inhibitors and 5-HT1A receptor antagonists. Treatment of substituted 2-chloroquinolines, including BioBlocks QU3501, with piperazine, 2-methyl-piperazine or 1,4-diazepane produced a set of amines which were further alkylated with (R)-(8-methyl-2,3-dihydro-[1,4]dioxino[2,3-f]quinolin-2-yl)methyl-4-bromobenzenesulfonate to yield the desired inhibitors.
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| 4. |
Sabine Kolczewski, Claus Riemer, Lucinda Steward, Juergen Wichmann, Thomas Woltering
Quinolines
In this Hoffmann-La Roche set of patents, scientists disclose a series of 5-HT5A receptor antagonists which are suggested as potentially useful in the prevention and/or treatment of depression, anxiety, schizophrenia and other related CNS disorders. Treatment of BioBlocks QU3502 with amines at elevated temperatures or by microwave heating afforded substituted 2-amino-6-chloroquinolines. A second treatment with amines under palladium mediated coupling conditions led to the desired substituted 2,6-diamino-quinolines.
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