CAS: 27060-91-9; 10-Chloro-11B-(2-Fluorophenyl)-7-(2-Hydroxyethyl)-3,5-Dihydro-2H-[1,3]Oxazolo[3,2-D][1,4]Benzodiazepin-6-One

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CAS号540-51-2 2-溴乙醇 | CAS号105-36-2 溴乙酸乙酯 | CAS号102408-32-2 7-chloro-5-(2-f... | CAS号101489-22-9 N-(4-chloro-2-(...

📜7-Chloro-5-(2-Fluorophenyl)-1,4-Bis(2-Hydroxyethyl)-2-Oxo-2,3-Dihydro-1H-Benzo[e][1,4]Diazepin-4-Ium 以 乙醇,水 用作溶剂,化学反应生成氟恶唑兰
参考文献:Kinetics And Mechanism Of The Acid-Base Equilibrium Of Mexazolam And Comparison With Those Of Other Commercial Benzodiazepinooxazole Drugs.
标题:Kinetics And Mechanism Of The Acid-Base Equilibrium Of Mexazolam And Comparison With Those Of Other Commercial Benzodiazepinooxazole Drugs.
摘要:研究了美沙班(mexazolam),氯沙班(cloxazolam),氟沙班(haloxazolam)和氟噻班(flutazolam)的噻唑啉环开环和闭环反应,采用ph跳跃法,与之前报道的噻唑班(oxazolam)情况类似 [kurono Et Al.,Chem. Pharm. Bull.,33,1633 (1985)].美沙班基本上以单一异构体存在,既可以是顺式,也可以是反式(指的是3-甲基基团和11B-(2'-氯苯基)基团),与噻唑班的情况不同(噻唑班的顺式异构体/反式异构体比例约为1:1).在ph范围1-13内,Ph-速度曲线显示出两步反应.为了对这些曲线进行解释,我们提出了一种反应机制,包括通过动力学方法检测到的中间体,该中间体位于亚胺结构(噻唑啉环开环形式)和闭环形式之间.这些美沙班的动力学特性与其他苯二氮平噻唑类化合物的特性不同,这种差异是由于3-甲基基团的存在,而不是2'-氯原子的存在.根据适当的反应机制,确定了美沙班及其缺乏2'-氯的类似物(3-甲基化合物),氯沙班,氟沙班和氟噻班的内在速率常数.
Doi:10.1248/cpb.35.3831

专利信息

专利号:US-10005720-B2
优先权日:2013-04-05
标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same
发明人：SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L
权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL
摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.

专利号:US-7309799-B2
优先权日:2004-06-01
标 题:Methods for the synthesis of milnacipran and congeners thereof
发明人：BUCHWALD STEPHEN L; SWAGER TIMOTHY M; RARIY ROMAN V
权利人:COLLEGIUM PHARMACEUTICAL INC
摘要:One aspect of the present invention relates to methods for synthesizing milnacipran or congeners thereof. Another aspect of the present invention relates to asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof. The present invention also relates to methods for synthesizing intermediates useful in the non-asymmetric or asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof.

专利号:US-2005282898-A1
优先权日:2004-06-01
标 题 :Methods for the synthesis of milnacipran and congeners thereof

专利号:US-2016046560-A1
优先权日:2013-04-05
标题 :Compounds useful for the treatment of metabolic disorders and synthesis of the same

专利号:WO-2005118564-A2
优先权日:2004-06-01
标 题:Methods for the synthesis of milnacipran and congeners thereof