Protecting-group-free synthesis of a dual CCK1/CCK2 receptor antagonist

作者:Liu Jing; Deng Xiaohu*; Fitzgerald Anne E; Sales Zachary S; Venkatesan Hariharan; Mani Neelakandha S
来源:Organic and Biomolecular Chemistry, 2011, 9(8): 2654-2660.
DOI:10.1039/c0ob01004a

摘要

In our pursuit of an efficient, protecting-group-free synthesis of the dual CCK1/CCK2 receptor antagonist 1, we have developed chemoselective conditions for sulfonamide formation reaction in pure water and a PhNMe(2) mediated carboxamide formation, both in the presence of a carboxylic acid. Practical synthesis of an unnatural, chiral beta-aryl-alpha-amino acid is also described.

  • 出版日期2011