乙醚 以 1-Acetoxy-2-(4-Methyl-Piperazino)-Ethane,水 作为反应溶剂,以90%的收率获得产物4-甲基-1-哌嗪乙酸 参考文献:Prodrugs Of 5,5-Diphenylhydantoin As Antiepileptic And Antiarrhythmic Agents 标题:Prodrugs Of 5,5-Diphenylhydantoin As Antiepileptic And Antiarrhythmic Agents 摘要:本发明涉及一种具有通式(I)的产品,该产品是苯妥英的一种新型前药,以及其具有治疗可接受性的溶剂合物和加成盐.该产品的溶解度明显高于苯妥英本身.此外,令人惊讶的是,其水解速率远高于其他已知的苯妥英前药,使其特别适用于抗癫痫和抗心律失常药物.
专利号:US-4308206-A 优先权日:1980-03-17 标 题:Process for preparing derivatives of 5,11-dihydro-6h-pyrido[2,3-b][1,4]-benzodiazepin-6-one, and the final derivatives and synthesis intermediates obtained thereby 发明人:GERSZBERG SZEPSEL 权利人:MICROSULES ARGENTINA SA 摘要:This invention relates to a process for preparing derivatives of 5,11-dihydro-6H-pyrido[2,3-b][1,4]-benzodiazepin-6-one of general formula (I) ##STR1## in which R is hydrogen, halogen or methyl; n R 1 and R 2 are linear or branched C 2 -C 4 alkyl groups, which alternatively may be joined together to give a piperazine cycle which can be substituted in position 4 with a methyl, ethyl or benzyl group, n and their salts with organic and inorganic acids, characterised by comprising the following stages: n (a) reacting a compound of general formula (X), ##STR2## in which R has the meaning heretofore defined, with 2-cloro-3-amino-pyridine of formula (III) ##STR3## in the presence of polyphosphoric acid, to give an intermediate of general formula (II) ##STR4## (b) reacting said intermediate with a compound of general formula (XI) ##STR5## in which R 1 and R 2 have the meaning heretofore defined and R 3 is a hydroxyl or halogen, in an inert solvent at a maximum temperature equal to the solvent boiling point, to give said derivatives of general formula (I). n The invention also relates to the final compounds thus obtained, and the synthesis intermediates obtained during the course of said process. n The final products of formula (I) are of great interest in the pharmaceutical field.
专利号:US-7935658-B2 优先权日:2003-12-17 标 题 :Methods for synthesis of encoded libraries
专利号:US-2011251089-A1 优先权日:2003-12-17 标题:Methods for synthesis of encoded libraries
专利号:US-4363816-A 优先权日:1981-02-02 标 题 :Tricyclic pyrroles, their compositions and their use 发明人:SENN-BILFINGER JOERG 权利人:BYK GULDEN LOMBERG CHEM FAB 摘要:1,4,9,10-tetrahydropyrrolo[3,2-b][1,5]benzodiazepin-10-ones have been found to provide excellent protection for the stomach and intestines of warm-blooded animals. They are useful for the treatment and prophylaxis of such maladies as gastritis, acute and chronic ulcus ventriculi and hyperacid gastric irritation. The compounds are administered enterally or parenterally, usually in a standard dosage form. The disclosure includes key intermediates, methods of synthesis, compositions and use.