926922-18-1Relevant articles and documents
High Turnover Pd/C Catalyst for Nitro Group Reductions in Water. One-Pot Sequences and Syntheses of Pharmaceutical Intermediates
Gallou, Fabrice,Li, Xiaohan,Lipshutz, Bruce H.,Takale, Balaram S.,Thakore, Ruchita R.
, p. 8114 - 8118 (2021/10/25)
Commercially available Pd/C can be used as a catalyst for nitro group reductions with only 0.4 mol % Pd loading. The reaction can be performed using either silane as a transfer hydrogenating agent or simply a hydrogen balloon (μ1 atm pressure). With this technology, a series of nitro compounds was reduced to the desired amines in high chemical yields. Both the catalyst and surfactant were recycled several times without loss of reactivity.
KINASE INHIBITORS AND USES THEREOF
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Page/Page column 44; 45, (2020/10/21)
This invention described herein relates to compounds of general formula (I) : (I), in which variable groups are as defined herein, and to their preparation and use. Uses for the compounds and for compositions containing them include treatment of cancer and other diseases mediated by protein kinases, such as Bcr-Abl kinase, and mutants thereof, such as the T315I mutant.
Hybrid pyrimidine alkynyls inhibit the clinically resistance related Bcr-AblT315I mutant
Lu, Xiaoyun,Zhang, Zhang,Ren, Xiaomei,Pan, Xiaofeng,Wang, Deping,Zhuang, Xiaoxi,Luo, Jingfeng,Yu, Rongmin,Ding, Ke
, p. 3458 - 3463 (2015/08/06)
abstract A series of pyrimidine alkynyl derivatives were designed and synthesized as new Bcr-Abl inhibitors by hybriding the structural moieties from GNF-7, ponatinib and nilotinib. One of the most potent compounds 4e strongly suppresses Bcr-AblWT and Bcr-AblT315I kinase with IC50 values of 5.0 and 9.0 nM, and inhibits the proliferation of K562 and murine Ba/F3 cells ectopically expressing Bcr-AblT315I cells with IC50 values of 2 and 50 nM, respectively. It also displays good pharmacokinetics properties with an oral bioavailability of 35.3% and T1/2 value of 48.7 h, and demonstrates significantly suppression on tumor growth in xenografted mice of K562 and Ba/F3 cells expressing Bcr-AblT315I. These inhibitors may serve as lead compounds for further developing new anticancer drugs overcoming the clinically acquired resistance against current Bcr-Abl inhibitors.
