| Literature DB >> 20977279 |
Christopher M Mapes1, Neelakandha S Mani, Xiaohu Deng, Chennagiri R Pandit, Kelly J McClure, Marna C W Pippel, Clark A Sehon, Laurent Gomez, Shirin Shinde, J Guy Breitenbucher, Todd K Jones.
Abstract
We describe a practical and scalable route to compound (Z)-1, a selective CCK1 receptor antagonist. Notable features of this concise route are (1) a regioselective construction of the pyrazole core through the reaction of an aryl hydrazine and an elaborated acetylenic ketone, (2) a Tf2O/pyridine mediated Z-selective dehydration of an α-hydroxyester, and (3) a stereoselective hydrolysis. The sequence is high-yielding and amenable for large-scale synthesis.Entities:
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Year: 2010 PMID： 20977279 DOI： 10.1021/jo1017684
Source DB: PubMed Journal: J Org Chem ISSN： 0022-3263 Impact factor: 4.354