CAS: 906673-45-8; 4-(4-Bromo-3-(Hydroxymethyl)Phenoxy)Benzonitrile

上下游产品

4-(4-bromo-3-formaldehydephenoxy)benzonitrile 2-bromo-5-hydroxybenzaldehyde 4-fluorobenzonitrile (2-bromo-5-hydroxybenzene)methanol

4-(4-溴-3-甲酰基苯氧基)苯甲腈 反应生成 2-溴-5-(4-氰基苯氧基)苄醇
参考文献:Boron-Containing Small Molecules
标题:Boron-Containing Small Molecules
摘要:本发明涉及用于治疗真菌感染的化合物,更具体地用于治疗甲真菌病和/或皮肤真菌感染的局部治疗.本发明涉及对真菌活性的化合物,并具有使化合物在与患者接触时能够到达受真菌感染的皮肤,指甲,头发,爪子或蹄部位的特定部位的性质.特别地,本发明的化合物具有物理化学性质,有助于穿透指甲板.

专利信息

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.