25015-63-8 = 144432-80-4 + 912844-88-3 反应条件:1.1 Catalysts: [[1,3-Bis[2,6-Bis(1-Methylethyl)Phenyl]-2-Phenyl-1H-Imidazolium-4,5-Diyl]-1,2-Ph...; 24 H,100 °C 标题:Nickel-Catalyzed C(Sp2)-H Borylation Of Arenes 作者:Das,Arpan; Hota,Pradip Kumar; Mandal,Swadhin K. 参考文献:Organometallics 日期:2019 卷标:38(17) 页码:3286-3293]
73183-34-3 = 144432-80-4 + 912844-88-3 反应条件:1.1 Catalysts: 2756816-84-7; 72 H,110 °C 标题:Rhodium Indenyl Nhc And Fluorenyl-Tethered Nhc Half-Sandwich Complexes: Synthesis,Structures And Applications In The Catalytic C-H Borylation Of Arenes And Alkanes 作者:Evans,Kieren J.; Morton,Paul A.; Luz,Christian; Miller,Callum; Raine,Olivia; Et Al 参考文献:Chemistry - A European Journal 日期:2021 卷标:27(71) 页码:17824-17833
专利号:WO-2018115362-A1 优先权日:2016-12-22 标 题 :Process for preparing 4-[(1-hydroxy-1,3-dihydro-2,1-benzoxaborol-5-yl)oxy]benzonitrile (crisaborole) 发明人:HUGUET CLOTET JUAN; OZORES VITURRO LÃ?DIA; RODRÃ?GUEZ ROPERO SERGIO; DALMASES BARJOAN PERE 权利人:LABORATORIOS LESVI SL 摘要:The present invention relates to a new one-pot synthesis employing 4-(4-bromo-3-(hydroxymethyl)phenoxy)benzonitrile (compound B) for preparing (4-[(1-hydroxy-1,3-dihydro-2,1-benzoxaborol-5-yl)oxy]benzonitrile (crisaborole) and pharmaceutically acceptable salts thereof in high yield and high purity. The novel process of the present invention is particularly suitable for industrial scale manufacture of crisaborole and its salts with excellent purity and good yields. The present invention also describes an intermediate, 4-(3-formyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenoxy)benzonitrile (compound I), which is inter alia suitable for preparing (4-[(1-hydroxy-1,3-dihydro-2, 1-benzoxaborol-5-yl)oxy]benzonitrile (crisaborole) and pharmaceutically acceptable salts thereof, as well as a another process suitable for industrial scale applications, employing the intermediate compound I in the preparation of crisaborole and pharmaceutically acceptable salts thereof, in high yield and high purity.