1037210-93-7Relevant academic research and scientific papers
A Design of Experiments Approach to a Robust Final Deprotection and Reactive Crystallization of IPI-926, A Novel Hedgehog Pathway Inhibitor
Martinot, Theodore A.,Austad, Brian C.,C?té, Alexandre,Depew, Kristopher M.,Genov, Daniel,Grenier, Louis,Helble, Joseph,Lescarbeau, Andre,Nair, Somarajan,Trudeau, Martin,White, Priscilla,Yu, Lin-Chen
, p. 1693 - 1702 (2015)
A design of experiments (DoE) approach was taken to optimize purity and reaction yield of the final debenzylation and hydrochloride salt formation of IPI-926. The study involved a careful dissection of the different process steps to enable an independent investigation of these steps while ensuring that process streams were representative. The results enabled a streamlined process from the final chemical transformation to the salting and isolation and led to the elimination of variability in the process as well as a robust control of impurities. The optimized process was applied to production and demonstrated on the kilogram scale.
ENZYMATIC TRANSAMINATION OF CYCLOPAMINE ANALOGS
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Page/Page column 15; 85-86, (2011/02/24)
Provided are processes for the synthesis of amino analogues from ketone starting materials
Discovery of a potent and orally active hedgehog pathway antagonist (IPI-926)
Tremblay, Martin R.,Lescarbeau, André,Grogan, Michael J.,Tan, Eddy,Lin, Grace,Austad, Brian C.,Yu, Lin-Chen,Behnke, Mark L.,Nair, Somarajan J.,Hagel, Margit,White, Kerry,Conley, James,Manna, Joseph D.,Alvarez-Diez, Teresa M.,Hoyt, Jennifer,Woodward, Caroline N.,Sydor, Jens R.,Pink, Melissa,MacDougall, John,Campbell, Matthew J.,Cushing, Jill,Ferguson, Jeanne,Curtis, Michael S.,McGovern, Karen,Read, Margaret A.,Palombella, Vito J.,Adams, Julian,Castro, Alfredo C.
experimental part, p. 4400 - 4418 (2010/03/02)
Recent evidence suggests that blocking aberrant hedgehog pathway signaling may be a promising therapeutic strategy for the treatment of several types of cancer. Cyclopamine, a plant Veratrum alkaloid, is a natural product antagonist of the hedgehog pathwa
CYCLOPAMINE ANALOGS
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Page/Page column 59, (2008/12/07)
The invention provides novel derivatives of cyclopamine having the following formula.
