1,3-环己二酮(3)与醌单缩醛4和7的碱催化反应分别产生多环产物5和8,在4的情况下产生可变量的二苯并呋喃酮6。另一方面,从由ZnCl 2催化的3与双缩醛11的反应中分离出2-芳基环己二酮9(方案2)。用(CH 3 O)2 SO 2 / K 2 CO 3处理加合物8结果通过逆迈克尔反应裂解杂环,得到可靠的烯酮23,该烯酮通过选择性氢化进一步转化为24。8-乙酰氧基二苯并呋喃酮22可通过酸处理和乙酰化从方案8获得(方案4)。甲硅烷基醚27和35与醌单缩醛的反应非常复杂(方案6)。所需的芳基环己酮衍生物28和36以非常低的产率形成。在某些条件下(高温或强路易斯酸作为催化剂),单电子转移或加到烯缩醛而不是醌单缩醛的烯酮功能上变得占主导地位。结合该研究,已经制备并表征了敏感的2-甲氧基对对苯醌单缩醛15(方案3)和29(方案6)。
1,3-环己二酮(3)与醌单缩醛4和7的碱催化反应分别产生多环产物5和8,在4的情况下产生可变量的二苯并呋喃酮6。另一方面,从由ZnCl 2催化的3与双缩醛11的反应中分离出2-芳基环己二酮9(方案2)。用(CH 3 O)2 SO 2 / K 2 CO 3处理加合物8结果通过逆迈克尔反应裂解杂环,得到可靠的烯酮23,该烯酮通过选择性氢化进一步转化为24。8-乙酰氧基二苯并呋喃酮22可通过酸处理和乙酰化从方案8获得(方案4)。甲硅烷基醚27和35与醌单缩醛的反应非常复杂(方案6)。所需的芳基环己酮衍生物28和36以非常低的产率形成。在某些条件下(高温或强路易斯酸作为催化剂),单电子转移或加到烯缩醛而不是醌单缩醛的烯酮功能上变得占主导地位。结合该研究,已经制备并表征了敏感的2-甲氧基对对苯醌单缩醛15(方案3)和29(方案6)。
[EN] PRODRUGS OF OXAZOLIDINONE CETP INHIBITORS<br/>[FR] PROMÉDICAMENTS D'INHIBITEURS DE CETP À BASE D'OXAZOLIDINONE
申请人:MERCK SHARP & DOHME
公开号:WO2010039474A1
公开(公告)日:2010-04-08
The compounds of Formula I are prodrugs of CETP inhibitors having a central oxazolidinone ring. The compounds cyclize by the elimination of HX to form an oxazolidinone ring after administration to a patient.
A method wherein lignocellulosic biomass materials are converted into combustible fuel products. In particular, the method is a continuous process. involving wet oxidation or steam explosion, for fermentatively converting such biomass materials into ethanol using a process design that permits all or part of the process water from the ethanol fermentation process to be recycled to reduce the consumption of process water. The effluent from the ethanol fermentation step may be subjected to an anaerobic fermentation step generating methane and a water effluent in which the amount of potentially inhibitory substances is at a sub-inhibitory level, which in turn permits all or part of the effluent water from the anaerobic fermentation step to be recycled into the process.
The compounds of Formula I are pro-drugs of CETP inhibitors having a central oxazolidinone ring. The compounds cyclize by the elimination of HX to form an oxazolidinone ring after administration to a patient.
The compounds of Formula I are pro-drugs of CETP inhibitors having a central oxazolidinone ring. The compounds cyclize by the elimination of HX to form an oxazolidinone ring after administration to a patient.
A method of forming a stable chromophore derived from vanylmandelic acid and the use thereof in the determination of vanylmandelic acid
申请人:Nassar, Michael Fouad
公开号:EP0045647A2
公开(公告)日:1982-02-10
The invention provides a method of forming a stable chromophore derived from vanylmandelic acid characterised by forming an ethyl acetate extract of a diazo derivative of vanylmandelic acid and adding dimethyl-sulphoxide and 2-amino-2-methyl-1-propanol to said extract. The diazo derivative may be the reaction product of p-nitrobenzenediazonium salt and vanylmandelic acid. The invention also includes a method of determining vanylmandelic acid characterised by forming a stable chromophore by the above method and quantitatively determining said stable chromophore. The method is particularly useful for the determining of urinary vanylmandelic acid.