Synthesis and pharmacological properties of 1,2-bis(fluoromethoxy)-1,1,3,3,3-pentafluoropropane
作者:Jan A. Ruzicka、James B. Hrdy、Max T. Baker
DOI:10.1016/0022-1139(95)03318-5
日期:1995.12
(compound B), a fluorinated diether derived from the anesthetic sevoflurane, was reacted with bromine trifluoride. With proper control of reaction temperature, a single product, 1,2-bis(fluoromethoxy)-1,1,3,3,3-pentafluoropropane (BFPP), was obtained in 58% yield. In the rat model, BFPP exhibited enhanced metabolic stability both in vivo and in liver microsomal preparations, evidenced by a reduction in
使氟甲基2-甲氧基-2,2-二氟-1-(三氟甲基)-乙基醚(化合物B)(一种衍生自麻醉的七氟醚的氟化二醚)与三氟化溴反应。在适当控制反应温度的情况下,以58%的产率获得了单一产物1,2-双(氟甲氧基)-1,1,3,3,3-五氟丙烷(BFPP)。在大鼠模型中,BFPP在体内和肝脏微粒体制剂中均表现出增强的代谢稳定性,这可通过减少氟化物的释放来证明。当静脉内给药时,化合物B和BFPP在该动物中均是镇静剂/催眠药。给予BFPP的动物的睡眠时间大约是同等剂量的化合物B的动物的睡眠时间的六倍。