CAS: 33034-67-2; 2-Chloro-4-(Trifluoromethyl)Pyrimidine

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241164-09-0 1261629-31-5 16097-64-6

上下游产品

CAS号179756-91-3 1-(4-三氟甲基嘧啶-2-基)哌嗪

2-羟基-4-三氟甲基嘧啶置于三氯氧磷体系中,化学反应 4.0H,以61%的收率获得2-氯-4-三氟甲基嘧啶
参考文献:电子不足的杂芳烃盐:氧化中过氧化氢活化的有机催化工具
标题:电子不足的杂芳烃盐:氧化中过氧化氢活化的有机催化工具
摘要:制备了一系列的单取代的嘧啶鎓和吡嗪鎓三氟甲磺酸酯和3,5-二取代的吡啶鎓三氟甲磺酸酯,并使用硫氧化作为模型反应,对过氧化氢的简单氧化催化剂进行了测试.它们的催化效率在很大程度上取决于取代基的类型,并且对于具有吸电子基团的衍生物而言是显着的,其反应性与黄酮盐相当,后者是氧合作用的主要有机催化剂.由于它们的高稳定性和非常好的可及性,4-(三氟甲基)嘧啶鎓和3,5-二硝基吡啶鎓三氟甲磺酸盐是选择的催化剂,并显示出催化脂肪族和芳香族硫化物氧化为亚砜的作用,定量转化率高,制备产率高,并且具有优异的性能.化学选择性.K R +值(p K R + <5)和较小的负还原电位(e Red >-0.5 V).在催化氧化过程中原位形成的过氧化氢加合物充当底物氧化剂.通过在b3Lyp / 6-311 ++ G(d,P)水平上的计算获得的从这些杂环氢过氧化物到硫代苯甲醚的转移的吉布斯自由能表明,它们是比烷基氢过氧化
Doi:10.1021/jo502865F

专利信息

专利号:US-9861636-B2
优先权日:2014-04-29
标题 :Polyfluorinated compounds acting as bruton tyrosine kinase inhibitors
发明人：HE WEI
权利人:HE WEI; ZHEJIANG DTRM BIOPHARMA CO LTD
摘要:Described herein is a novel series of multi-fluoro-substituted pyrazolopyrimidine compounds or salts thereof. These compounds are Bruton's tyrosine kinase (BTK) inhibitors. These compounds may possess better BTK inhibition selectivity and pharmacokinetic properties. Disclosed herein are the synthesis methods of these compounds. Disclosed herein are novel synthesis methods of the multi-fluoro-substituted benzophenone and substituted phenoxy benzene. Also disclosed are pharmaceutical compositions comprising the BTK inhibitors described herein. The present invention also relates to pharmaceutical formulations comprising the compounds described herein as active ingredients. The present invention also includes the therapeutic methods by administering the BTK inhibitors and their formulations to treat and inhibit autoimmune disease, hypersensitivity disease, inflammatory diseases and cancer.