40016-69-1Relevant articles and documents
Synthesis of β-Lactams by Palladium(0)-Catalyzed C(sp3)?H Carbamoylation
Dailler, David,Rocaboy, Ronan,Baudoin, Olivier
, p. 7218 - 7222 (2017/06/13)
A general and user-friendly synthesis of β-lactams is reported that makes use of Pd0-catalyzed carbamoylation of C(sp3)?H bonds, and operates under stoichiometric carbon monoxide in a two-chamber reactor. This reaction is compatible with a range of primary, secondary and activated tertiary C?H bonds, in contrast to previous methods based on C(sp3)?H activation. In addition, the feasibility of an enantioselective version using a chiral phosphonite ligand is demonstrated. Finally, this method can be employed to synthesize valuable enantiopure free β-lactams and β-amino acids.
Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinyl carbamates as potent and long acting muscarinic antagonists
Prat, Maria,Buil, María Antonia,Fernández, Maria Dolors,Castro, Jordi,Monleón, Juan Manuel,Tort, Laia,Casals, Gaspar,Ferrer, Manuel,Huerta, Josep Maria,Espinosa, Snia,López, Manuel,Segarra, Victor,Gavald, Amadeu,Miralpeix, Montserrat,Ramos, Israel,Vilella, Dolors,González, Marisa,Córdoba, Mnica,Cárdenas, Alvaro,Antón, Francisca,Beleta, Jorge,Ryder, Hamish
, p. 3457 - 3461 (2011/06/24)
Novel quaternary ammonium derivatives of N,N-disubstituted (3R)-quinuclidinyl carbamates have been identified as potent M3 muscarinic antagonists with long duration of action in an in vivo model of bronchoconstriction. These compounds have also presented a high level of metabolic transformation (human liver microsomes). The synthesis, structure-activity relationships and biological evaluation of these compounds are reported.