专利号:US-2023339844-A1 优先权日:2020-09-17 标题:A process for the synthesis of anthranilic acid/amide compounds and intermediates thereof 发明人:MAHAPATRA TRIDIB; PATRA PRANAB KUMAR; KLAUSENER ALEXANDER G M; MAL SANJIB; SHARMA RAJU 权利人:PI INDUSTRIES LTD; PI INDUSTRIES LTD 摘要:The present invention disclosed a process for the synthesis of compound of formula (Z) or a salt thereof, n n n n n n n n n n wherein, R, R 1 , R 2 , R 3 and R 10 are as defined in the detailed description. The process further comprises the synthesis of an anthranilic diamide compound of formula (I).
专利号:US-8212077-B2 优先权日:2008-08-05 标 题:Process for the synthesis of agomelatine 发明人:HARDOUIN CHRISTOPHE; LECOUVE JEAN-PIERRE; BARAGNIER NICOLAS 权利人:HARDOUIN CHRISTOPHE; LECOUVE JEAN-PIERRE; BARAGNIER NICOLAS; SERVIER LAB 摘要:Process for the industrial synthesis of the compound of formula (I)
专利号:EP-1363951-B1 优先权日:2000-12-07 标 题 :Polynuclear complex fe(iii) with pullulan oligomers, process of its obtaining, and pharmaceutical preparations on the basis of the complex 发明人:ILIC LJUBOMIR; RISTIC SUZANA; CAKIC MILORAD; NIKOLIC GORAN; STANKOVIC SLOBODAN 权利人:AD ZDRAVLJE FARMACEUTSKO HEMIJ 摘要:A polynuclear complex of pullulan oligomers of formula (I): wherein n = (100-8200), obtained by process of synthesis of soluble pullulan with insoluble iron (III)-hydroxyde of formula (II): wherein n=(900). The process of synthesis is characterized by technical simplicity and economy. In accordance with suggested process, first of all, preparation of pullulan for synthesis, including its characterization (determination of RG, Mw, Mn, [θ]) is carried out, and subsequently its hydrogenation is carried out in order to eliminate reducing groups, iron(III)-hydroxyde gel is prepared, and synthesis of the complex can start. Obtained complex is afterwards prepared for pharmacological use and it is subjected to the subsequent physical and chemical processes of purification. The preparation obtained in such a way is used for prevention and treatment of syderopenic anemia in human and veterinay medicine.
专利号:WO-2013001322-A1 优先权日:2011-06-30 标 题:PROCESS FOR THE SYNTHESIS OF (5α,17β)-N-[(2,5-BIS(TRIFLUOROMETHYL)-PHENYL]-3-OXO-4-AZA-5-ANDROST-1-ENE-17-CARBOXAMIDE 发明人:SOEROES BELA; TUBA ZOLTAN; GALIK GYOERGY; MAHO SANDOR; BALOGH LASZLO; VINCZE PETER; HORVATH JANOS; KOVACS ANDRAS; BENI ZOLTAN; VARGA FRIGYES 权利人:RICHTER GEDEON NYRT; SOEROES BELA; TUBA ZOLTAN; GALIK GYOERGY; MAHO SANDOR; BALOGH LASZLO; VINCZE PETER; HORVATH JANOS; KOVACS ANDRAS; BENI ZOLTAN; VARGA FRIGYES 摘要:The synthesis consists of reaction steps as follows: oxidizing the α,β-unsaturated ketone system of ring 'A' of pregn-4-ene-3,20-dion- of formula (II) with sodium metaperiodate in tert-butanol in the presence of potassium permanganate and alkali metal carbonate, reacting the obtained 3,5-seco acid with an ester of chloroformic acid in the presence of tertier organic base below 0°C, reacting the obtained new compound after isolation or without isolation with ammonia or ammonium acetate, cyclization of the resulting carboxamides with an acid, cathalytic hydrogenating the obtained ene lactame, and oxidizing the side chain at position 17 of the obtained pregnane compound with an alkali metal hypobromide in aqueous dioxane below 10°C. Thereafter on one hand the obtained (5α,17β)-3-oxo-4-aza-5-androstane-17-carboxylic acid is reacted with chloroformic acid ester, the obtained new compound is reacted with 2,5-bis(trifluoromethyl)-aniline in the presence of a Lewis acid, the obtained amide is reacted with trimethyl chlorosilane in inert atmosphere in the presence of Î?,Î?,Î?',Î?'-tetramethyl-ethylendiamine, then en excess iodine is added to the reaction mixture and the product of the iodination reaction is crystallized from acetonitrile, then the obtained 2-iodo-3-oxo-4-aza-17β-carboxamide is reacted with potassium tert-butylate to furnish final product. On the other hand, (5α,17β)-3-oxo-4-aza-5-androstane-17-carboxylic acid is transformed into methylester by known method, this latter is transformed into methyl (2α,5α,17β)-2-iodo-3-oxo-4-aza-5-androstane-17-carboxylate according to known method, the obtained compound is reacted with potassium-tert-butylate, the obtained (5α,17β)-3-oxo-4-aza-5-androst-1-ene-17-carboxylic acid is reacted with an ester of chloroformic acid, then the obtained new compound is coupled with 2,5-bis(trifluoromethyl)-aniline in the presence of a Lewis acidcatalyst to gain final product.
专利号:US-4777257-A 优先权日:1983-08-25 标题:Certain tetrahydronaphthyl or indanylcarboxylates and derivatives thereof which inhibit the synthesis of thromboxane 发明人:KANAO MUNEFUMI 权利人:DAIICHI SEIYAKU CO 摘要:Benzocycloalkane derivatives of the formula (I) ##STR1## wherein: Z represents a methylene group or an ethylene group, either one of R 1 and R 2 represents --(CH 2 ) m --COOR 3 and the other represents ##STR2## wherein R 3 represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms, n represents an interger of 1 to 6 and m represents an interger of 0 to 5, and the physiologically acceptable salts thereof; having a strong and selective inhibition activity of thromboxane A 2 synthesis.
专利号:US-6207863-B1 优先权日:1998-08-11 标题 :Synthesis of haloformimine compounds 发明人:BERRIER JOHN VINCENT; UMARVADIA ASHUTOSH SUMANTRAI 权利人:ROHM & HAAS 摘要:Disclosed is an improved method for the preparation of highly pure haloformimine compounds in high yields by reacting a formimine compound in a solvent with a halogenating agent while maintaining the pH of the halogenation reaction in the range of 2 to 5. The pH of the reaction may be maintained by a variety of means, such as by the addition of a base.
参考文献:10.1007/bf01952278 摘要:Loriette C, Pierre Y, Chatagner F. Effect of dietary cholic acid and cholesterol on liver and kidney cystathionase and cysteine sulfinate decarboxylase activities and taurine concentrations in the rat. Cellular and Molecular Life Sciences. 1980 Mar;36(3):285–6. doi: 10.1007/bf01952278. 参考文献:10.1007/s002449910001 摘要:Ueno H, Oishi K, Sayato Y, Nakamuro K. Oxidative Cell Damage in Kat-Sod Assay of Oxyhalides as Inorganic Disinfection By-Products and Their Occurrence by Ozonation. Archives of Environmental Contamination and Toxicology. 2000 Jan 01;38(1):1–6. doi: 10.1007/s002449910001. 参考文献:10.1007/bf02160621 摘要:Laarhoven WH, Nivard RJF, Havinga E. Estrogenic activity and steric hindrance to coplanarity of alkyl substituted 4,4′-dimethoxystilbenes. Cellular and Molecular Life Sciences. 1961 May;17(5):214–5. doi: 10.1007/bf02160621. 参考文献:10.1007/s00726-004-0097-1 摘要:Olszanecki R, Marcinkiewicz J. Taurine chloramine and taurine bromamine induce heme oxygenase-1 in resting and LPS-stimulated J774.2 macrophages. Amino Acids. 2004 Aug;27(1):29–35. doi: 10.1007/s00726-004-0097-1.