专利号:EP-2703383-A1 优先权日:2012-08-27 标 题:Process for the preparation of agomelatine 发明人:BAROZZA ALESSANDRO; VERONESE MARTINO; ROLETTO JACOPO; PAISSONI PAOLO 权利人:PROCOS SPA 摘要:Disclosed is a process for the synthesis of Agomelatine (1), N-(2-(7-methoxynaphthalen-1-yl)ethyl)acetamide from ethyl 2-(7-methoxynaphthalen-1-yl)acetate (4).n n Said synthesis method is particularly advantageous compared with known procedures because it uses low-cost reagents under mild reaction conditions and allows the isolation of a product with excellent yields and quality.
专利号:US-5907058-A 优先权日:1998-07-29 标题:Synthesis of an acid addition salt of delta-aminolevulinic acid from 5-bromo levulinic acid esters 发明人:MOENS LUC 权利人:MIDWEST RESEARCH INST 摘要:A process of preparing an acid addition salt of delta-aminolevulinic acid comprising: n dissolving a lower alkyl 5-bromolevulinate and an alkali metal diformylamide in an organic solvent selected from the group consisting of acetonitrile, methanol, tetrahydrofuran, 2-methyltetrahydrofuran and methylformate or mixtures thereof to form a suspension of an alkyl 5-(N,N-diformylamino) levulinate ester; and hydrolyzing said alkyl 5-(N,N-diformylamino) levulinate with an inorganic acid to form an acid addition salt of delta-amino levulinic acid.
专利号:US-6583317-B1 优先权日:2000-10-18 标 题 :Synthesis of acid addition salt of delta-aminolevulinic acid from 5-bromo levulinic acid esters 发明人:MOENS LUC 权利人:MIDWEST RESEARCH INST 摘要:A process of preparing an acid addition salt of delta-aminolevulinc acid comprising:a) dissolving a lower alkyl 5-bromolevulinate and hexamethylenetetramine in a solvent selected from the group consisting of water, ethyl acetate, chloroform, acetone, ethanol, tetrahydrofuran and acetonitrile, to form a quaternary ammonium salt of the lower alkyl 5-bromolevulinate; andb) hydrolyzing the quaternary ammonium salt with an inorganic acid to form an acid addition salt of delta-aminolevulinic acid.
专利号:EP-0522956-B1 优先权日:1991-07-08 标 题 :Preparation of 2-(2-thienyl) ethylamine and synthesis of thieno [3,2-C] pyridine derivatives therefrom 发明人:HARRINGTON PETER J; SANCHEZ IGNACIO H 权利人:SANOFI SA 摘要:Compounds of the formulae: and wherein: R<1>, R<2>, R<3> and R<4> are independently hydrogen, lower alkyl of one to six carbon atoms, aryl or substituted aryl; are advantageously converted to isocyanurate compounds, 2-(2-thienyl)ethylamine compounds and thieno[3,2-c]pyridine derivatives and the pharmaceutically acceptable salts thereof, particularly ticlopidine hydrochloride.
专利号:US-2022259212-A1 优先权日:2019-07-11 标题:Inhibitors of indoleamine 2,3-dioxygenase and/or tryptophan 2,3-dioxygenase 发明人:BOSS CHRISTOPH; CREN SYLVAINE; KIMMERLIN THIERRY; LOTZ-JENNE CARINA; POTHIER JULIEN; TIDTEN-LUKSCH NAOMI 权利人:IDORSIA PHARMACEUTICALS LTD 摘要:The present invention relates to compounds of Formula (I) inhibiting indoleamine 2,3-dioxygenase (IDO) and/or tryptophan 2,3-dioxygenase (TDO) enzymes. Further, their synthesis and their use as medicaments in the treatment of inter alia cancer is disclosed.
专利号:US-8981092-B2 优先权日:2008-09-19 标题 :Substituted 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-ones as modulators of protein kinase activity 发明人:MIRIZZI DANILO; CERVI GIOVANNI; D ANELLO MATTEO; PAPEO GIANLUCA MARIANO ENRICO; FERGUSON RON; CASUSCELLI FRANCESCO 权利人:MIRIZZI DANILO; CERVI GIOVANNI; D ANELLO MATTEO; PAPEO GIANLUCA MARIANO ENRICO; FERGUSON RON; CASUSCELLI FRANCESCO; NERVIANO MEDICAL SCIENCES SRL 摘要:Compounds which are 4,7-disubstituted derivatives of 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-one compounds, n nor pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.