CAS: 269409-73-6; 3-(4,4,5,5-Tetramethyl-1,3,2-Dioxaborolan-2-yl)Benzoic Acid

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CAS号25015-63-8 频那醇硼烷 | CAS号618-51-9 间碘苯甲酸 | CAS号76-09-5 频哪醇 | CAS号25487-66-5 3-羧基苯硼酸 | CAS号99-05-8 间氨基苯甲酸 | CAS号73183-34-3 双戊酰二硼 | CAS号480425-35-2 3-甲氧羰基苯硼酸频哪醇酯 | CAS号618-89-3 3-溴苯甲酸甲酯 | CAS号1073353-62-4 3-(哌啶-1-羰基)苯硼酸频哪酯 | CAS号380151-86-0 3-甲酰基苯硼酸频哪醇酯 | CAS号840521-76-8 N-(2-(二甲基氨基)乙基)... | CAS号618-51-9 间碘苯甲酸 | CAS号1073353-61-3 3-(1-吡咯烷基羰基)苯硼酸频哪醇酯 | CAS号1048647-68-2 3-(苯甲氨基羰基)苯硼酸频哪酯 | CAS号943911-66-8 N-(2-羟乙基)-3-(4,...

3-甲氧羰基苯硼酸频哪醇酯置于lithium Hydroxide体系中,用 四氢呋喃,水 用作溶剂,化学反应 18.0H,以73%的收率获得3-羧基苯硼酸频那醇酯
参考文献:内部路易斯酸辅助的苯甲酸催化
标题:内部路易斯酸辅助的苯甲酸催化
摘要:摘要 引入内部路易斯酸辅助的苯甲酸衍生物作为新型的低分子量单氢键供体催化剂,用于硝基烯烃的活化.所选的2-硼基苯甲酸衍生物通过将吲哚添加到硝基烯烃中,可以得到非常好的产物收率.对照实验表明,内部路易斯酸配位和羧酸官能度对于这些催化剂的最佳性能都是至关重要的. 引入内部路易斯酸辅助的苯甲酸衍生物作为新型的低分子量单氢键供体催化剂,用于硝基烯烃的活化.所选的2-硼基苯甲酸衍生物通过将吲哚添加到硝基烯烃中,可以得到非常好的产物收率.对照实验表明,内部路易斯酸配位和羧酸官能度对于这些催化剂的最佳性能都是至关重要的.
Doi:10.1055/s-0031-1291048

专利信息

专利号:US-7122694-B2
优先权日:1998-11-06
标 题 :Hydroboronation process
发明人：MARCUCCIO SEBASTIAN MARIO; RODOPOULOS MARY; WEIGOLD HELMUT
权利人:BORON MOLECULAR PTY LTD
摘要:The invention relates to processes for the synthesis of aryl or alkene borates which comprises reacting: (i) an olefinic compound having a halogen or halogen-like substituent in a vinylic substitution position, or (ii) an aromatic ring having a halogen or halogen-like substituent in a ring substitution position, with a disubstituted monohydroborane in the presence of a Group 8-11 metal catalyst. The invention also relates to the use of these borates in coupling reactions. The invention further relates to certain disubstituted monohydroboranes and aryl or alkene borates.

专利号:WO-2024131948-A1
优先权日:2022-12-22
标题 :Method for preparing p2x3 inhibitor
发明人：ZHANG XUEJUN; ZANG YANG; LI QUN; ZHANG BO; LI YUAN; YANG QIONGFENG; XIA QINGFENG; YUE YANG; YANG JUN; LI LIE
权利人:HUMANWELL HEALTHCARE GROUP CO LTD; WUHAN HUMANWELL INNOVATIVE DRUG RES AND DEVELOPMENT CENTER LIMITED COMPANY
摘要:The present invention belongs to the field of drug synthesis. Specifically, disclosed is a method for preparing a P2X3 inhibitor, i.e., 2-fluoro-5-(((2S,3R)-3-hydroxybutan-2-yl)oxy)-3(5-methylthiazol-2-yl)-N-((R)-1-(2-(trifluoromethyl)pyrimidin-5-yl)ethyl)benzamide (I-1). The method comprises the following steps: using 3-bromo-2-fluoro-5-iodobenzoic acid as a starting material, substituting iodine with a hydroxyl group and subjecting a carboxyl group to methyl esterification to obtain a compound 1C; subjecting the compound 1C and B2(pin)2 to a coupling reaction to obtain 1D; subjecting the compound 1D and 2-bromo-5-methylthiazole to a coupling reaction to obtain 1E; substituting the compound 1E with 1F to then obtain a compound 1H; hydrolyzing 1H under the action of a base to obtain 1I, and subjecting the compound 1I and 1L to a condensation reaction to obtain a product I-1. The synthesis route provided by the present invention makes it easy to control product quality, has a high yield and is suitable for industrial production.