478833-25-9Relevant academic research and scientific papers
Execution of a performic acid oxidation on multikilogram scale
Ripin, David H. Brown,Weisenburger, Gerald A.,Am Ende, David J.,Bill, David R.,Clifford, Pamela J.,Meltz, Clifford N.,Phillips, James E.
, p. 762 - 765 (2007)
In order to run a peracid oxidation on multikilogram scale in a pilot plant facility with an acceptable level of risk, an extensive study of the thermal characteristics of the reaction, reactants, and quench was undertaken. A number of features were engineered into the process in order to confidently run the process without the potential for a thermal or pressure excursion on scale.
Route development and bulk synthesis of CP-865,569
Belecki, Katherine,Berliner, Martin,Bibart, Richard Todd,Meltz, Cliff,Ng, Karl,Phillips, James,Ripin, David H. Brown,Vetelino, Michael
, p. 754 - 761 (2012/12/29)
The synthesis of zwitterionic CP-865,569 by three different synthetic routes is described. The first two routes differ in the method of introducing the sulfonic acid at the penultimate step: by sulfite displacement of a benzylic chloride and by oxidation of a benzylic thioacetate. The third route is a convergent route to the drug candidate. The synthesis strategy was primarily driven by the need to introduce the sulfonic acid functionality at the final stage of the synthesis due to the high water solubility and low organic solubility of the desired product.
Piperazinyl CCR1 antagonists-optimization of human liver microsome stability
Brown, Matthew F.,Bahnck, Kevin B.,Blumberg, Laura C.,Brissette, William H.,Burrell, Sara A.,Driscoll, James P.,Fedeles, Flavia,Fisher, Michael B.,Foti, Robert S.,Gladue, Ronald P.,Guzman-Martinez, Aikomari,Hayward, Matthew M.,Lira, Paul D.,Lillie, Brett M.,Lu, Yi,Lundquist, Greg D.,McElroy, Eric B.,McGlynn, Molly A.,Paradis, Timothy J.,Poss, Christopher S.,Roache, James H.,Shavnya, Andrei,Shepard, Richard M.,Trevena, Kristen A.,Tylaska, Laurie A.
, p. 3109 - 3112 (2008/03/13)
The synthesis, biological activity, and pharmacokinetic profile of CCR1 antagonists are described.
AMORPHOUS UND CRYSTAL FORMS OF (5-CHLORO-2-{2-
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Page 14; 25, (2008/06/13)
This invention relates to amorphous and crystal salt forms of (5-chloro-2-{2-[4-(4-fluoro--benzyl)-(2R,5S)-2,5-dimethyl-piperazin-1-yl]-2-oxo-ethoxy)-phenyl)-methanesulfonic acid, useful in treating or preventing a disorder or condition by antagonizing th
Novel sulfonic acid derivatives
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, (2008/06/13)
A compound of the formula or the pharmaceutically acceptable salt thereof; wherein X, Y, a, b, c, d, R1, R2, R3 and R5 are as defined above useful to treat inflammation and other immune disorders.
