PYRAZOLO[1,5a]PYRIMIDINE DERIVATIVES AS IRAK4 MODULATORS
申请人:Arora Nidhi
公开号:US20120015962A1
公开(公告)日:2012-01-19
Compounds of the formula I or II:
wherein X, m, Ar, R
1
and R
2
are as defined herein. The subject compounds are useful for treatment of IRAK-mediated conditions.
Pyrazolo[1,5a]pyrimidine derivatives as IRAK4 modulators
申请人:Hoffmann-La Roche Inc.
公开号:US09255110B2
公开(公告)日:2016-02-09
Compounds of the formula I or II:
wherein X, m, Ar, R1 and R2 are as defined herein. The subject compounds are useful for treatment of IRAK-mediated conditions.
PYRAZOLO[1,5A]PYRIMIDINE DERIVATIVES AS IRAK4 MODULATORS
申请人:F. Hoffmann-La Roche AG
公开号:EP3252054A1
公开(公告)日:2017-12-06
Compounds of the formula I or II:
wherein X, m, Ar, R1 and R2 are as defined herein. The subject compounds are useful for treatment of IRAK-mediated conditions.
式 I 或 II 的化合物:
其中 X、m、Ar、R1 和 R2 如本文所定义。上述化合物可用于治疗 IRAK 介导的病症。
Improved Suzuki-Miyaura Reactions of Aryldiazonium Salts with Boronic Acids by Tuning Palladium on Charcoal Catalyst Properties
Abstractmagnified imageAn improved Suzuki–Miyaura cross‐coupling reaction of aryldiazonium tetrafluoroborates with boronic acids catalyzed by a highly active palladium catalyst supported on charcoal is described as an extremely practical and efficient protocol. A properties‐activity study of various catalysts clearly established that the optimal catalytic activity was obtained with palladium nanoparticles having a low oxidation degree and uniformly dispersed on the charcoal. The optimized reaction conditions allow the cross‐coupling to proceed at room temperature without any base and ligand in technical grade methanol. Although the catalyst could not be recycled, the low palladium contamination of the solvent and product after a simple filtration of the palladium on charcoal (Pd/C) renders the present protocol competitive and safer for the environment compared to more conventional homogeneous conditions. We have highlighted the efficiency of this novel protocol by a short synthesis of the fungicide Boscalid®.
PYRAZOLO[1,5A]PYRIMIDINE AND THIENO[3,2B]PYRIMIDINE DERIVATIVES AS IRAK4 MODULATORS