Process for preparing 1-bromoalkylbenzene derivatives and intermediates thereof
申请人:SUMITOMO CHEMICAL COMPANY LIMITED
公开号:EP0637580A1
公开(公告)日:1995-02-08
A 1-bromoalkylbenzene derivative is prepared by reacting a phenylalkene derivative with hydrogen bromide in the presence of a non-polar solvent. The phenylalkene derivative is prepared by reacting an alkenyl halide with metal magnesium to form a Grignard reagent, and then reacting the Grignard reagent with a benzyl halide derivative. An allyl Grignard reagent is prepared by reacting continuously an allyl halide derivative with metal magnesium in an organic solvent, in which the allyl halide derivative and metal magnesium are continuously added to the reaction system and the allyl Grignard reagent formed is continuously removed from the reaction system. The processes provide the intended compounds in high yields, high selectivities and high purities.
1-bromoalkylbenzene derivative is prepared by reacting a phenylalkene derivative with hydrogen bromide in the presence of a non-polar solvent.苯基烷烃衍生物的制备方法是先使烯基卤化物与金属镁反应生成格氏试剂,然后使格氏试剂与苄基卤化物衍生物反应。烯丙基格氏试剂是通过烯丙基卤化物衍生物与金属镁在有机溶剂中连续反应制备的,其中烯丙基卤化物衍生物和金属镁被连续加入反应体系,形成的烯丙基格氏试剂被连续从反应体系中移除。这些工艺可提供高产率、高选择性和高纯度的预期化合物。
DRUG FOR PREVENTION OR TREATMENT OF DIABETES
申请人:Kowa Company, Ltd.
公开号:EP1747780A1
公开(公告)日:2007-01-31
The present invention provides a medicine for preventing or treating a diabetes, which includes 2,2-dichloro-12-(4-chlorophenyl)-dodecanoic acid or a pharmacologically acceptable salt thereof, and glibenclamide as active ingredients. The present invention provides a method for preventing or treating a diabetes, which includes administering 2,2-dichloro-12-(4-chlorophenyl)-dodecanoic acid or a pharmacologically acceptable salt thereof, and glibenclamide to a patient suffering from or having a possibility of suffering from diabetes.
The present invention provides a medicine for preventing or treating a diabetes, which includes 2,2-dichloro-12-(4-chlorophenyl)-dodecanoic acid or a pharmacologically acceptable salt thereof, and glibenclamide as active ingredients. The present invention provides a method for preventing or treating a diabetes, which includes administering 2,2-dichloro-12-(4-chlorophenyl)-dodecanoic acid or a pharmacologically acceptable salt thereof, and glibenclamide to a patient suffering from or having a possibility of suffering from diabetes.
In screening experiments certain omega-substituted alkyl carboxylic acids were found to produce an increase in insulin-stimulated C-14-acetate incorporation into triglycerides, which may indicate an improvement in the action of insulin. Antidiabetic and lipid-lowering properties in genetically diabetic ob/ob mice demonstrated the in vivo relevance of the insulin-potentiating effects seen in vitro. The chemical structures of the w-substituted alkyl carboxylic acids with insulin-potentiating effects correspond to the general formula ring-spacer-COOH. A close structure-activity relationship was observed. The most potent compound in ob/ob mice was 3e, which normalized blood glucose as well as hyperinsulinaemia and lowered serum triglycerides and cholesterol by 52% and 37%, respectively. On the basis of these results, omega-substituted alkyl carboxylic acids are interesting as a new class of oral antidiabetic agents with insulin-sensitizing and lipid-lowering activity. (C) Elsevier, Paris.