CAS: 497832-99-2; 4-Bromo-1-Methyl-3-(Trifluoromethyl)-1H-Pyrazole

相似化合物

1089212-38-3 721402-02-4 2248269-53-4

上下游产品

methylhydrazine 1-methyl-3-trifluoromethylpyrazol 1-methyl-3-(trifluoromethyl)-1H-pyrazole-4-carboxylic acid 4-bromo-1-methyl-3-trifluoromethyl-5-pyrazolecarboxylic acid [1-methyl-3-(trifluoromethyl)-1H-pyrazol-5-yl]boronic acid (1-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl)boronic acid

1-甲基-3-三氟甲基-1H-吡唑置于n-溴代丁二酰亚胺(Nbs)体系中,用 N,N-二甲基甲酰胺 作为反应溶剂,化学反应 10.0H,以92%的收率获得产物1-甲基-3-三氟甲基-4-溴-1H-吡唑
参考文献:官能化的1-甲基-3 / 5-(三氟甲基)-1 H-吡唑的实用合成方法
标题:官能化的1-甲基-3 / 5-(三氟甲基)-1 H-吡唑的实用合成方法
摘要:一种新的,高产且实用的合成1-甲基-3-(三氟甲基)-1H-吡唑和1-甲基-5-(三氟甲基)-1H-吡唑的重要实用方法到药物和农业化学的发展.从4-乙氧基-1,1,1-三氟-3-丁烯-2-一开始,提出了一步合成目标吡唑区域异构混合物的步骤.此混合物的分离步骤,阐述了沸点的基础上vs压力图分析.证明了在第3和第5位带有cf 3基团的区域异构结构单元的有效合成策略.一组1-甲基-3-(三氟甲基)-1 H基于1-甲基-3-(三氟甲基)-1 H-吡唑的锂化反应,合成了含有醛,酸,松果酸硼酸,亚磺酸锂和磺酰氯等官能团的β-吡唑.nbs在温和的条件下对1-甲基-3-(三氟甲基)-1 H-吡唑和1-甲基-5-(三氟甲基)-1 H-吡唑进行溴化.在1-甲基-5-(三氟甲基)-1 H的4位上引入官能团通过在适当的溴化物中进行br-Li交换,优化了相应的醛和酸的合成,说明了吡唑.或者,基于4-溴的直接原位金属
DOI:10.1021/acs.Oprd.0C00300

专利信息

专利号:US-9925177-B2
优先权日:2015-01-22
标题:4-methylsulfonyl-substituted piperidine urea compounds
发明人：OSLOB JOHAN; AUBELE DANIELLE; KIM JAE; MCDOWELL ROBERT; SONG YONGHONG; SRAN ARVINDER; ZHONG MIN
权利人:MYOKARDIA INC
摘要:The present invention provides novel 4-methylsulphone-substituted piperidine urea compounds that are useful for the treatment of dilated cardiomyopathy (DCM) and conditions associated with left and/or right ventricular systolic dysfunction or systolic reserve. The synthesis and characterization of the compounds is described, as well as methods for treating DCM and other forms of heart disease.

专利号:US-8445510-B2
优先权日:2010-05-14
标题 :Fused bicyclic kinase inhibitors
发明人：MULVIHILL MARK J; STEINIG ARNO G; CREW ANDREW PHILIP; JIN MEIZHONG; KLEINBERG ANDREW; LI AN-HU; WANG JING
权利人:MULVIHILL MARK J; STEINIG ARNO G; CREW ANDREW PHILIP; JIN MEIZHONG; KLEINBERG ANDREW; LI AN-HU; WANG JING; OSI PHARMACEUTICALS LLC
摘要:Compounds of Formula I, as shown below and defined herein: n n n n n n n n n n pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven at least in part by at least one of RON, MET or ALK. This Abstract is not limiting of the invention.

专利号:US-11123337-B2
优先权日:2015-01-22
标题 :4-methylsulfonyl-substituted piperidine urea compounds
发明人：OSLOB JOHAN; AUBELE DANIELLE; KIM JAE; MCDOWELL ROBERT; SONG YONGHONG; SRAN ARVINDER; ZHONG MIN
权利人:MYOKARDIA INC
摘要:The present invention provides novel 4-methylsulphone-substituted piperidine urea compounds that are useful for the treatment of dilated cardiomyopathy (DCM) and conditions associated with left and/or right ventricular systolic dysfunction or systolic reserve. The synthesis and characterization of the compounds is described, as well as methods for treating DCM and other forms of heart disease.