专利号:WO-2025086625-A1 优先权日:2023-10-26 标题 :Synthesis method for deuterated tinidazole 发明人:MEI SHU; GUO HUI; CHEN WULIAN 权利人:ANPEL LABORATORY TECH SHANGHAI INC 摘要:The present invention relates to a synthesis method for a deuterated tinidazole. The deuterated tinidazole is as represented by formula I, wherein one or more of R 1 -R 5 are deuterium, and the rest is hydrogen. The synthesis method comprises the step of oxidizing an intermediate B with m-chloroperoxybenzoic acid to prepare the deuterated tinidazole, wherein the oxidation is carried out under low-temperature and alkaline conditions; and the intermediate B is as represented by formula II. By using the synthesis method of the present invention, the problems of deuterium shedding and isotope dilution in the reaction process can be avoided, and the stable isotope-labeled deuterated tinidazole with the isotope abundance of > 98% is obtained with a higher yield. The prepared deuterated tinidazole can be used as an isotope internal standard reagent for the quantitative detection of tinidazole, which, for example, can be used to detect residual tinidazole in meat products by means of an isotope internal standard method, and has the advantages of having high recovery efficiency from a matrix, and being environmentally friendly and safe.
专利号:US-2007060558-A1 优先权日:2004-07-30 标 题 :Hybrid molecules QA where Q is an aminoquinoline and A is an antibiotic residue, the synthesis and uses thereof as antibacterial agents 发明人:SANCHEZ MURIEL; MEUNIER BERNARD 权利人:CENTRE NAT RECH SCIENT 摘要:The invention concerns an aminoquinoline-antibiotic hybrid compound of general formula (I): Q—(Y 1 ) p —(U) p —(Y 2 ) p -A: wherein Q represents an aminoquinoline, (Y 1 ) p (U) p —(Y 2 ) p″ is an optional spacer and A is an antibiotic residue. The invention enables the antibiotic residue activity to be unexpectedly enhanced.
专利号:US-8129544-B2 优先权日:2002-10-15 标题:1-substituted-4-nitroimidazole compound and method for preparing the same 发明人:GOTO FUMITAKA; TAKEMURA NORIAKI; OTANI TADAAKI; HASEGAWA TAKESHI; TSUBOUCHI HIDETSUGU; UTSUMI NAOTO; FUJITA SHIGEKAZU; KURODA HIDEAKI; SHITSUTA TAKUYA; SASAKI HIROFUMI 权利人:GOTO FUMITAKA; TAKEMURA NORIAKI; OTANI TADAAKI; HASEGAWA TAKESHI; TSUBOUCHI HIDETSUGU; UTSUMI NAOTO; FUJITA SHIGEKAZU; KURODA HIDEAKI; SHITSUTA TAKUYA; SASAKI HIROFUMI; OTSUKA PHARMA CO LTD 摘要:The present invention relates to a 1-substituted-4-nitroimidazole compound represented by the general formula (1) or a salt thereof, n n(wherein R is a hydrogen atom, a lower alkoxy group-substituted lower alkyl group, a phenyl-lower alkoxy group-substituted lower alkyl group, a cyano-substituted lower alkyl group, a phenyl-lower alkyl group which may have lower alkoxy groups as the substituents in the phenyl ring or a group of the formula —CH 2 R A ; X is a halogen atom or a group of the formula —S(O)n-R 1 ) and method for preparing the same. The compound of the formula (1) is a useful compound as an intermediate for synthesis of various pharmaceutical and agricultural chemicals, particularly, as intermediates for antitubercular agents.
专利号:US-6518266-B1 优先权日:1999-07-22 标题:1- Aryl-3-thioalkyl pyrazoles, the synthesis thereof and the use thereof as insecticides 发明人:DHANOA DALJIT S; DOLLER DARIO; MEEGALLA SANATH; SOLL RICHARD M; WISNEWSKI NANCY; SILVER GARY; STINCHCOMB DAN T; SEWARD R LEE; AGRAFIOTIS DIMITRIS; SHA DEYOU 权利人:DIMENSIONAL PHARMACEUTICALS 3; HESKA CORP 摘要:The present invention is directed to novel pyrazole derivatives and their use as pesticidal agents. The pyrazole derivatives have Formula I:or a salt thereof, whereR1 represents R5O, R5SO2, R5SO or R5S in which R5 is as defined herein;X is halo, cyano, C1-6 alkoxycarbonyl, C2-6 alkynyl, optionally substituted C6-14 aryl or an optionally substituted 5- to 7-membered heteroaromatic ring linked to thiazole via a carbon-carbon bond;R2 is hydrogen, amino, chloro, bromo, iodo, cyano, C1-6 alkoxy, C1-6 alkyl or C6-10 aryl; andR3-R7 each represent hydrogen, halogen, straight- or branched-chain C1-4 alkyl or C1-4 alkoxy, either of which is unsubstituted or substituted by one or more halogen atoms, straight- or branched-chain C1-4 alkylthio or C1-4 alkylsulphinyl, either of which is substituted by one or more halogen atoms, nitro, cyano, or straight- or branched-chain C1-4 alkylsulphonyl group which is unsubstituted or substituted by one or more halogen atoms.
专利号:US-3644392-A 优先权日:1969-05-12 标 题:1-substituted-5-nitroimidazole-2-carboximidates 发明人:HENRY DAVID W 权利人:MERCK & CO INC 摘要:1-SUBSTITUTED - 5 - NITROIMIDAZOLE-2-CARBOXIMIDATES AND 1-SUBSTITUTED - 5 - NITROIMDAZOLE - 2 -CARBOXYLIC ACID ESTERS ARE PREPARED FROM 2-SUBSTITUTED - 5 - NITROMIDAZOLES BY TREATING A 1-SUBSTITUTED-2-CYANO - 5 -NITROIMIDAZOLE WITH BASE AND BY REACTING A 1-SUBSTITUTED-2-CYANO-5-NITROIMIDAZOLE WITH A LOWER ALKANOL IN THE PRESENCE OF BASE AND TREATING THE PRODUCT FORMED WITH A MINERAL ACID. THE 1SUBSTITUTED-5-NITROIMIDAZOLE-2-CARBOXYLIC ACID ESTERS AND THE 1-SUBSTITUTED - 5 - NITROIMIDAZOLE-2-CARBOXIMIDATES ARE USEFUL AS INTERMEDIATES IN THE SYNTHESIS OF BIOLOGICALLY ACTIVE 1-SUBSTITUTED-5-NITRIOMIDIDAZOLE-2-CARBOXAMIDES.
专利号:RU-2122542-C1 优先权日:1997-01-23 标 题:Method of synthesis of 2-(r)-4(5)-nitroimidazoles
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合成参考文献
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