Room-temperature direct alkenylation of 5-pyrazolones
A mild and efficient method for the direct alkenylation of 5-pyrazoles by Pd-catalyzed C-H bond activation is described. The reaction smoothly proceeds at room temperature to provide products in up to 92 % yield. Heterocycles containing the 5-pyrazolone moiety are synthesized by an oxidative Heck-type reaction. The direct alkenylation of 5-pyrazolones at room temperature through Pd-catalyzed C-H bond activation is described. Copyright
Yang, Yiwen,Gong, Hao,Kuang, Chunxiang
supporting information
p. 5276 - 5281
(2013/09/02)
Pyrazolone methylamino piperidine derivatives as novel CCR3 antagonists
The discovery and optimization of a novel class of potent CCR3 antagonists is described. Details of synthesis and SAR are given together with some ADME properties of selected compounds. An optimal balance between activities, physicochemical properties, and in vitro metabolic stability was reached by the proper choice of substituents.