专利号:WO-9837078-A1 优先权日:1997-02-20 标题 :Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes 发明人:DOERWALD FLORENCIO ZARAGOZA 权利人:NOVO NORDISK AS 摘要:A solid phase method for the synthesis of a plurality of differently substituted thiophenes with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The thiophenes are prepared by reaction of a substrate-bound primary or secondary amine with a thiophosgene equivalent and reaction of the resulting intermediate with an acceptor-substituted acetonitrile in the presence of a base. Alkylation with an appropriate alkyl halide, followed by Thorpe-Ziegler-cyclization yields differently substituted, support-bound 3-aminothiophenes. These may be screened on the substrate or cleaved from the substrate and then screened in solution. Alternatively, the resin-bound 3-amino thiophenes or the synthetic intermediates can be subjected to further synthetic transformations (N-acylation, reduction) on the support, which permits the preparation of further therapeutically interesting compounds. The efficient synthesis of a wide variety of thiophenes using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiophene-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.
专利号:US-10968174-B2 优先权日:2016-12-21 标题:Synthesis of a thiosulfonic acid by a step of periodate mediated oxidative coupling of a thiosulfonic acid with an aniline 发明人:SINCLAIR JAMES PETER; NICOLL SARAH LOUISE; STOREY JOHN MERVYN DAVID; LARCH CHRISTOPHER PAUL 权利人:WISTA LAB LTD 摘要:The present invention pertains generally to the field of chemical synthesis, and more particularly to methods for the chemical synthesis of a thiosulfonic acid of Formula (1) by a step of periodate mediated oxidative coupling of a thiosulfonic acid of Formula (2) with an aniline of Formula (3), as described herein. The present invention also relates to such methods which incorporate one or more additional (subsequent and/or preceding) steps, for example, to prepare compounds of Formula (5) from compounds of Formula (1); to prepare compounds of Formula (6) from compounds of Formula (5); and to prepare compounds of Formula (2) from compounds of Formula (4), as described herein.
专利号:US-2025205370-A1 优先权日:2022-03-19 标 题:Synthesis of toluidine blue o and a kit for mucosal application 发明人:PANDA SWAGATIKA 权利人:PANDA SWAGATIKA 摘要:The present invention describes synthesis of Toluidine blue O for a formulation to be used for screening and biopsy site identification in oral cancer. The invention discloses two formulations and a method of delivery of the said formulations via a kit. The method described is a reproducible method of synthesis of pharmaceutical grade Toluidine blue O of acceptable purity and good colorimetric value. The present invention also discloses a kit that includes one formulation of a cleaning solution containing an organic acid and another formulation that is a vital stain formulation. The kit is packaged as a dual chamber sprayer having two pump dispensers, that facilitates ready to use, convenient dental chair side delivery, and allows mass screening.
专利号:US-7173021-B2 优先权日:2004-09-02 标题:Synthesis of temozolomide esters as potent anticancer pro-drugs for topical and transdermal applications in treatments of cancers 发明人:WANG YONGFENG; CONWAY BARBARA R; SUPPASANSATORN PANASSAYA 权利人:TIANJIN NORTH PHARM SCI TECH C 摘要:This invention relates to the use of temozolomide esters (4-dihydro-3-methyl-4-oxoimidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxylate esters) Formula 1 as potent anticancer pro-drugs for treatment of cancers by topical and transdermal applications, and to a novel process for synthesis of temozolomide esters by a direct esterification of temozolomide acid (3,4-dihydro-3-methyl-4-oxoimidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxylic acid) with a halogeno-aliphatic compound in presence of a base, or with an alcohol in presence of a dehydrate agent
专利号:US-6448446-B1 优先权日:2000-01-12 标 题 :Synthesis of N,N-disubstituted-p-phenylenediamine 发明人:TANG LI; TAN YUYING 权利人:ANTICANCER INC 摘要:An improved synthesis of N,N,-disubstituted-p-phenylene-diamine (DSPDA) preferably di-n-butyl-p-phenylenediamine is disclosed. The improvement rests on the discovery that DSPDA and its salts are extremely sensitive to oxygen so that once the product DSPDA or its salt is formed, oxygen must be excluded from all manipulations.
专利号:US-5416189-A 优先权日:1992-11-04 标 题:Process for the synthesis of polyamides 发明人:VANDEVIJVER ERIC; GAUTHY FERNAND; MOMTAZ ARDECHIR 权利人:SOLVAY 摘要:Process for the synthesis of polyamides by polycondensation in a closed reactor of one or a number of dicarboxylic acids with a diamine compound containing not less than 60 mol % of-m-xylyenediamine, in which all the amount of diamine compound stoichiometrically necessary for the polycondensation reaction is quickly brought into contact with the molten acid, the temperature of the reaction mixture is raised to a value greater than the melting point of the polyamide produced, the pressure is only allowed to rise to a value sufficient to prevent solidification of the reaction mixture and a substantial loss of diamine compound and, at the end of the reaction, the pressure of the reaction mixture is reduced and the polyamide formed is recovered.
参考文献:10.1002/cbdv.201100043 摘要:Damien Dorman HJ, Shikov AN, Pozharitskaya ON, Hiltunen R. Antioxidant and Pro‐Oxidant Evaluation of a Potentilla alba L. Rhizome Extract. Chemistry & Biodiversity. 2011 Jul;8(7):1344–56. doi: 10.1002/cbdv.201100043.