1-氯-4-氟苯置于2,2,6,6-四甲基哌啶,硼酸三异丙酯,正己基锂体系中,用 四氢呋喃,正己烷 作为反应溶剂,化学反应 5.0H,以90%的收率获得产物5-氯-2-氟苯硼酸 参考文献:The Expedient Synthesis Of 4,2'-Difluoro-5'-(7-Trifluoromethyl-Imidazo[1,2-A]Pyrimidin-3-yl)Biphenyl-2-Carbonitrile,A Gaba α2/3 Agonist 标题:The Expedient Synthesis Of 4,2'-Difluoro-5'-(7-Trifluoromethyl-Imidazo[1,2-A]Pyrimidin-3-yl)Biphenyl-2-Carbonitrile,A Gaba α2/3 Agonist 摘要:An Expedient Regioselective Synthesis Of A Gaba Alpha 2/3 Agonist 1 Is Described. The Key Step Is An Efficient Regioselective Palladium-Catalyzed Coupling Of 7-Trifluoromethylimidazo[1,2A] Pyrimidine (5) To 5'-Chloro-4,2'-Difluorobiphenyl-2-Carbonitrile (15). The Efficiency Of This Step Was Affected By The Choice Of Solvent,Ligand,And Tetrabutylammonium Salt Additive. DOI:10.1021/op050217J
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.
参考文献:10.1055/s-0036-1588303 摘要:Rossi R, Bellina F, Lessi M, Manzini C, Marianetti G. Direct (Hetero)arylation Reactions of (Hetero)arenes as Tools for the Step- and Atom-Economical Synthesis of Biologically Active Unnatural Compounds Including Pharmaceutical Targets. Synthesis. 2016 Oct 11;48(22):3821–62. doi: 10.1055/s-0036-1588303.