CAS: 444120-91-6; (6-Chloropyridin-3-yl)Boronic Acid

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5-溴-2-氯吡啶置于正丁基锂,硼酸三异丙酯体系中,用 乙醚 作为反应溶剂,以87%的收率获得产物2-氯-5-吡啶硼酸
参考文献:新型卤代吡啶基硼酸和酯的合成.第1部分:6-卤代吡啶-3-基硼酸和酯
标题:新型卤代吡啶基硼酸和酯的合成.第1部分:6-卤代吡啶-3-基硼酸和酯
摘要:本文介绍的新的6-卤代吡啶-3-基-硼酸和酯的合成和分离的一般方法2-5.制备这些化合物时考虑到了从2,5-二卤代吡啶开始的与三烷基硼酸酯的区域选择性卤素金属交换.迄今为止研究的所有底物均提供单一的区域异构硼酸或酯产物.另外,已经发现这些化合物与一系列的芳基卤化物进行了pd催化的偶联,并授权了一种制备新吡啶库的策略.
DOI:10.1016/s0040-4020(02)00152-7

专利信息

专利号:US-12150934-B2
优先权日:2016-11-30
标 题 :Methods of using substituted pyrazole and pyrazole compounds and for treatment of hyperproliferative diseases
发明人：SIDDIQUI ARSHAD M; CIBLAT STEPHANE; CONSTANTINEAU-FORGET LEA; GRAND-MAITRE CHANTAL; GUO XIANGYU; SRIVASTAVA SANJAY; SHIPPS GERALD W; COOPER ALAN B; OZA VIBHA; KOSTURA MATTHEW W; LUTHER MICHAEL; LEVINE JEDD
权利人:BANTAM PHARMACEUTICAL LLC
摘要:Disclosed are methods of treating hyperproliferative disorders such as cancer, methods of arresting the cell cycle in cancer cells, methods of inhibiting glutathione synthesis in cancer cells, and associated compounds for use and uses in medicaments. In certain embodiments, the methods, uses and compounds are provided with reference to compounds of the structural formula (I), in which X1, X2, Z1, Z2, the ring system denoted by “aâ€?, R1, L1, L2, Q, L3, R3, L4, R4, L5, and R5 are as described herein. In certain embodiments, compounds disclosed herein are especially active against cancers having a mutant KRAS gene.