6374-24-9Relevant academic research and scientific papers
Synthetic method of 1,3,4-thiadiazole derivative
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Paragraph 045; 0047, (2018/12/05)
The invention discloses a synthetic method of a 1,3,4-thiadiazole derivative. The method comprises the following steps: (1) using hydrazine hydrate as a raw material, under the action of a catalyst, reacting with acid, to obtain a hydrazide compound I; (2) using alkyl chloroformate and thiocyanate to react in a condition of a solvent, to obtain an isothiocyanate compound II; (3) in a reaction system of the isothiocyanate compound II, adding solution containing the compound I, reacting to obtain solution containing a compound III; (4) processing the solution of the compound III by dehydrating,neutralizing, and washing, to obtain a compound IV; (5) in the conditions of an acid-binding agent and a solvent, adding alkyl halide or sulfuric acid diester into the compound IV, reacting to obtaina compound V; and (6) enabling the compound V to perform an amination reaction with primary amine, to obtain the 1,3,4-thiadiazole derivative VI. The preparation method has the advantages of green andno pollution, simple and convenient operation, higher yield, mild reaction condition and the like.
Synthesis method of 2-amino-5, 8-dimethoxy[1, 2, 4]triazolo[1, 5-c]pyrimidine
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Paragraph 0011; 0027; 0028, (2017/01/02)
The invention discloses a synthesis method of 2-amino-5, 8-dimethoxy[1, 2, 4]triazolo[1, 5-c]pyrimidine (AMTP). 4-amino-2, 5-dimethoxy pyrimidine and phenoxy carbonyl isothiocyanate are adopted as the basic raw materials, under the action of a specific catalyst, nucleophilic addition, hydroxylamine substituttion, aromatic cyclization and other reactions are carried out to synthesize the product. The method innovatively selects phenoxy carbonyl structure compound as the substrate and significantly enhances the reaction rate. The method has the advantages of short reaction route, simple operation, mild reaction conditions, smooth operation, easy treatment of three wastes, and short full flow, thus having great industrial value.
Design and synthesis of indole, 2,3-dihydro-indole, and 3,4-dihydro-2H-quinoline-1-carbothioic acid amide derivatives as novel HCV inhibitors
Kang, Iou-Jiun,Wang, Li-Wen,Hsu, Sheng-Ju,Lee, Chung-Chi,Lee, Yen-Chun,Wu, Yen-Shian,Hsu, Tsu-An,Yueh, Andrew,Chao, Yu-Sheng,Chern, Jyh-Haur
scheme or table, p. 4134 - 4138 (2010/04/26)
An efficient synthetic methodology to provide indole, 2,3-dihydro-indole, and 3,4-dihydro-2H-quinoline-1-carbothioic acid amide derivatives is described. These conformationally restricted heterobicyclic scaffolds were evaluated as a novel class of HCV inhibitors. Introduction of an acyl group at the NH2 of the thiourea moiety has been found to enhance inhibitory activity. The chain length and the position of the alkyl group on the indoline aromatic ring markedly influenced anti-HCV activity. The indoline scaffold was more potent than the corresponding indole and tetrahydroquinoline scaffolds and analogue 31 displayed excellent activity (EC50 = 510 nM) against HCV without significant cytotoxicity (CC50 >50 μM).
NOVEL 2,3-BENZODIAZEPINE DERIVATIVES AND THEIR USE AS ANTIPSYCHOTIC AGENTS
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Page/Page column 42-43, (2008/12/04)
Disclosed are novel 2, 3 -benzodiazepine of formula (I), wherein R9 and R10 are alkoxy derivatives, methods of making the same, and their use in treating psychotic disorders. FIG. 1 shows, comparatively, the effect of clozapine, compound 121 and compound
Isothiazole derivatives useful as anticancer agents
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, (2008/06/13)
The present invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein X1, R1, R2and R3are as defined herein. The invention also relates to pharmaceutical compositions containing the above compounds and to methods treating hyperproliferative disorders in mammals by administering the above compounds.
Novel process of alkoxy and aryloxy isothiocyanate preparation
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, (2008/06/13)
Alkoxy and aryloxy isothiocyanates are produced by the reaction of a haloformate and an alkali or alkaline earth metal thiocyanate in the presence of water and a catalyst comprising a six membered mononuclear or ten membered fused polynuclear aromatic, heterocyclic compound having 1 or 2 nitrogen atoms as the only hetero atoms in the ring.
Process for the production of isothiocyanate derivatives
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, (2008/06/13)
Derivatives of alkoxy, aryloxy and alkene isothiocyanates are produced by the reaction of a haloformate, an alkali, alkaline earth metal, lead or ammonium thiocyanate and a compound having the formula R1 YH wherein R1 is alkyl, aryl or alkoxy, Y is oxygen, sulfur or NR2 and R2 is hydrogen or R1, in the presence of a solvent or water and a catalyst.
