DirectC(sp(3))-Hborylation of amides, ureas, and 2-aminopyridine derivatives at the position α to the N atom, which gives the corresponding α-aminoalkylboronates, has been achieved with a heterogeneous catalyst system consisting of [Rh(OMe)(cod)]2 and a silica-supported triarylphosphine ligand (Silica-TRIP) that features an immobilized triptycene-type cage structure with a bridgehead P atom. The
The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.
Substituted Guanidines: Introducing Diversity in Combinatorial Chemistry
作者:Montserrat del Fresno、Ayman El-Faham、Louis A. Carpino、Miriam Royo、Fernando Albericio
DOI:10.1021/ol006322p
日期:2000.11.1
[GRAPHICS]The guanidine moiety is an important motif present in many biologically active compounds. Fully substituted guanidines are of key importance for the development of bioactive molecules. The present paper reports on an efficient procedure for the direct solid phase conversion of amines to fully substituted guanidines under very mild conditions.