Process development of CP-481715, a novel CCR1 antagonist
Process development for the synthesis of 2-quinoxalinecarboxamide, N-[(1S,2S,4R)-4-(aminocarbonyl)-1-[(3-fluorophenyl)-methyl]-2, 7-dihydroxy-7-methyloctyl] is described. An optimized and streamlined process starting from lactone 2 was developed: Lactone
Li, Bryan,Andresen, Brian,Brown, Matthew F.,Buzon, Richard A.,Chiu, Charles K.-F.,Couturier, Michel,Dias, Eric,Urban, Frank J.,Jasys, V. John,Kath, John C.,Kissel, William,Le, Tung,Li, Z. Jane,Negri, Joanna,Poss, Christopher S.,Tucker, John,Whritenour, David,Zandi, Kathleen
p. 466 - 471
(2012/12/25)
CRYSTAL FORMS OF QUINOXALINE-2-CARBOXYLIC ACID [4-CARBAMOYL-1-(3-FLUOROBENZYL)-2,7-DIHYDROXY-7-METHYL-OCTYL]-AMIDE
The invention relates to crystal forms of quinoxaline-2-carboxylic acid [4-carbamoyl-1-(3-fluorobenzyl)-2,7-dihydroxy-7-methyl-octyl]-amide, useful in treating or preventing a disorder or condition by antogonizing the CCR1 receptor, and to their methods o
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Page 25
(2010/02/06)
Dihydoxyhexanoic acid derivatives, their intermediates, and methods of making
This invention relates to dihydroxyhexanoic acid derivatives and their intermediates, as well as to methods of preparing such compounds. Additionally, present invention relates to removing a protecting group from a protected amine wherein the method comprises reacting the protected amine with phosphoric acid.
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Page 16
(2010/02/05)
Novel CCR1 antagonists with improved metabolic stability
The synthesis, biological activity, and pharmacokinetic profile of novel CCR1 antagonists are described.
Brown, Matthew F.,Avery, Mike,Brissette, William H.,Chang,Colizza, Kevin,Conklyn, Maryrose,DiRico, Amy P.,Gladue, Ronald P.,Kath, John C.,Krueger, Suzanne S.,Lira, Paul D.,Lillie, Brett M.,Lundquist, Greg D.,Mairs, Erin N.,McElroy, Eric B.,McGlynn, Molly A.,Paradis, Timothy J.,Poss, Christopher S.,Rossulek, Michelle I.,Shepard, Richard M.,Sims, Jeff,Strelevitz, Timothy J.,Truesdell, Susan,Tylaska, Laurie A.,Yoon, Kwansik,Zheng, Deye
p. 2175 - 2179
(2007/10/03)
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