专利号:US-7420052-B2 优先权日:2001-08-24 标 题:Intermediates for synthesis of vinblastine, process for preparation of the intermediates and process for synthesis of vinblastines 发明人:FUKUYAMA TOHRU; TOKUYAMA HIDETOSHI; YOKOSHIMA SATOSHI 权利人:JAPAN SCIENCE & TECH AGENCY 摘要:An intermediate for vinblastine synthesis represented by general formula A. n ngeneral formula A.n n(in the formula, R 1 , R 2 , R 3 and R 4 are the group selected independently from the group consisting of H, lower alkyl group, lower alkoxy group, halogen, lower perfluoroalkyl group, lower alkylthio group, hydroxy group, amino group, mono- or di-alkyl or acylamino group, lower alkyl or arylsulfonyloxy group. R 5 is H, or a lower alkyl group or a substituted or non-substituted aryl group, R 6 is an alkyl group of carbon number 4 or less, R 7 is a substituted or non-substituted aryl group, R 8 is a substituted or non-substituted aryl group or lower alkyl group and R 9 is an acyl group or trialkylsilyl group.) A method for synthesis of the compound of general formula A utilizing radical ring forming reaction of thioanilides and using the compound of general formula B as the starting material, synthesizing thioanilide of general formula C by the reaction with compound 1 and the formation of a 11-membered ring by intramolecular alkylation of 2-nitrobenzenesulfonamide by which the reactions can proceed under mild conditions and high yield can be accomplished.
专利号:WO-2024105700-A1 优先权日:2022-11-18 标 题:A method for the synthesis of anthranilic amide compounds and intermediates thereof 发明人:MALVIYA NITIN; MAL SANJIB; KLAUSENER ALEXANDER G M 权利人:PI INDUSTRIES LTD 摘要:The present invention discloses a method for the synthesis of a compound of formula (V) or a salt thereof, wherein, R, R1, R2, R3, R4a and R4b are as defined in the detailed description. The method further comprises the synthesis of an anthranilic diamide compound of formula (Z).
专利号:WO-2025134140-A1 优先权日:2023-12-19 标题:A method for the synthesis of substituted anthranilic amide compounds, intermediates and salts thereof 发明人:MALVIYA NITIN JAIKANT; SINGH VIPENDER; SHAH JIGARKUMAR HARKISHANDAS; KALE MANOJ GANPAT; KAVITAKE SANTOSH GIRIDHAR; BORHADE AJIT SAHEBRAO; KLAUSENER ALEXANDER G M 权利人:PI INDUSTRIES LTD 摘要:The present invention discloses a method for the synthesis of compounds of formula (I) or a salt thereof, wherein, R is selected from hydrogen, halogen, cyano, C1-C12 alkyl, C1-C12 haloalkyl, C1-C12 alkoxy, C1-C12 haloalkoxy, or C3-C8 cycloalkyl; R4 is selected from hydrogen, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, C1-C12 haloalkyl, C2-C12 haloalkenyl, C2-C12 haloalkynyl, C1-C12 alkoxy, C1-C12 haloalkoxy, C3-C8 cycloalkyl, or C3-C8 cycloalkyl-C1-C10 alkyl; and n represents an integer selected from 0-4. The method further comprises the synthesis of an anthranilic diamide compound of formula (A).
专利号:WO-2025057193-A1 优先权日:2023-09-13 标题:A method for the synthesis of substituted anthranilic amide compounds, intermediates and salts thereof 发明人:MALVIYA NITIN JAIKANT; SINGH VIPENDER; KALE MANOJ GANPAT; SHAH JIGARKUMAR HARKISHANDAS; GAVHANE KISHOR BAPU; KAVITAKE SANTOSH GIRIDHAR; BORHADE AJIT SAHEBRAO; KLAUSENER ALEXANDER G M 权利人:PI INDUSTRIES LTD 摘要:The present invention provides a method for the synthesis of compounds of formula (I), intermediates, and salts thereof, formula (I) wherein, R, R1 and n are as described in the description. The method further comprises the synthesis of anthranilic diamide compounds of formula (E), wherein the formula (E) is described in the description.
专利号:US-4431828-A 优先权日:1982-11-10 标题 :Regeneration of 6-fluoro-4-chromanone from by-products in the synthesis of sorbinil 发明人:CUE JR BERKELEY W; HAMMEN PHILIP D; MASSETT STEPHEN S 权利人:PFIZER 摘要:6-Fluoro-4-chromanone, a sorbinil intermediate, is regenerated from enantiomeric and mixtures of enantiomeric and racemic compounds obtained as major by-products in the synthesis of sorbinil. The regenerated intermediate is useful in the synthesis of additional sorbinil.
专利号:US-4841045-A 优先权日:1985-03-12 标 题 :Synthesis of vinblastine and vincristine type compounds 发明人:KUEHNE MARTIN 权利人:UNIV VERMONT 摘要:A new process for the stereospecific synthesis of alkaloids of the vinblastine and vincristine type including the synthesis of vinblastine and vincristine as well novel alkaloids which are active as anti-tumor agents.
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