CAS: 221352-10-9; 3,3-Dimethylbenzo[c][1,2]Oxaborol-1(3H)-Ol

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CAS号5419-55-6 硼酸三异丙酯 | CAS号7073-69-0 2-(2-溴苯基)-2-丙醇 | CAS号67-64-1 丙酮 | CAS号610-94-6 2-溴苯甲酸甲酯 | CAS号244205-40-1 2-溴苯硼酸

📜2-苯基-2-丙醇置于正丁基锂,硼酸三异丙酯,Silver Carbonate体系中,用 正庚烷 用作溶剂,化学反应生成3,3-二甲基苯并[c][1,2]氧杂戊硼烷-1(3H)-醇
参考文献:一种3,3-二甲基苯并[c][1,2]氧杂戊硼烷-1 (3H)-醇的制备方法
标题:一种3,3-二甲基苯并[c][1,2]氧杂戊硼烷-1 (3H)-醇的制备方法
摘要:本发明涉及一种3,3‑二甲基苯并[c][1,2]氧杂戊硼烷‑1(3H)‑醇的制备方法,包括:在0~10oc条件下,将2‑苯基‑2‑丙醇与正丁基锂混合在正庚烷中,进行羟基的锂化,然后升温至40~60oc进行邻位碳原子的锂化;硼酸化;加入碳酸银进行分解反应,酸化水解后,对水相进行萃取,碱洗后,得到3,3‑二甲基苯并[c][1,2]氧杂戊硼烷‑1(3H)‑醇的钠盐分散相;酸化后,溶剂萃取后,减压浓缩得到3,3‑二甲基苯并[c][1,2]氧杂戊硼烷‑1(3H)‑醇.本发明提供了一种以2‑苯基‑2‑丙醇为原料制备3,3‑二甲基苯并[c][1,2]氧杂戊硼烷‑1(3H)‑醇的方法,所述方法选择了合适的锂化温度(0~10oc)得到了目标物,但同时副产物严重,而本发明选用了合适的后处理方法,将副产物酸化处理后,使其反应成目标物,由此提高了目标物的收率和纯度.

专利信息

专利号:US-8933018-B2
优先权日:2011-02-07
标题 :Boron containing polybasic bacterial efflux pump inhibitors and therapeutic uses thereof
发明人：GLINKA TOMASZ; HIGUCHI ROBERT; HECKER SCOTT; EASTMAN BRIAN; RODNY OLGA
权利人:GLINKA TOMASZ; HIGUCHI ROBERT; HECKER SCOTT; EASTMAN BRIAN; RODNY OLGA; REMPEX PHARMACEUTICALS INC
摘要:Disclosed herein are polybasic bacterial efflux pump inhibitors containing boronic acid functionality and their methods of synthesis, methods of use, and pharmaceutical compositions. Some embodiments include methods of treating or preventing a bacterial infection by co-administering to a subject infected with bacteria or at risk of infection with bacteria the efflux pump inhibitor with another anti-bacterial agent.