title: Protecting-group-free synthesis of a dual CCK1/CCK2 receptor antagonist.
abstract: 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 β-aryl-α-amino acid is also described.
authors.affiliation: Johnson & Johnson Pharmaceutical Research and Development, L.L.C. 3210 Merryfield Row, San Diego, CA 92121, USA.
authors.forename: Jing
authors.initials: J
authors.lastname: Liu
authors.forename: Xiaohu
authors.initials: X
authors.lastname: Deng
authors.forename: Anne E
authors.initials: AE
authors.lastname: Fitzgerald
authors.forename: Zachary S
authors.initials: ZS
authors.lastname: Sales
authors.forename: Hariharan
authors.initials: H
authors.lastname: Venkatesan
authors.forename: Neelakandha S
authors.initials: NS
authors.lastname: Mani
mesh_terms: D015394:Molecular Structure; D043886:Receptor, Cholecystokinin A / Q000037:antagonists & inhibitors*; D043887:Receptor, Cholecystokinin B / Q000037:antagonists & inhibitors*; D013237:Stereoisomerism
chemical_list: D043886:Receptor, Cholecystokinin A; D043887:Receptor, Cholecystokinin B