专利号:US-7939679-B2 优先权日:2006-01-19 标题:Method for synthesis of ciguatoxin CTX1B and compounds useful for the synthesis of ciguatoxin CTX1B 发明人:HIRAMA MASAHIRO; INOUE MASAYUKI 权利人:JAPAN SCIENCE & TECH AGENCY 摘要:Disclosed is a method for total synthesis of CTX1B, which is developed for the synthesis of a ciguatoxin analogue such as CTX3C and enables the more efficient application of an established reaction to the total synthesis of CTC1B. More specifically, disclosed is a method for total synthesis of CTX1B comprising; an O.S-acetal formation for synthesizing a novel compound (3); a radical cyclization reaction for constructing a 9-membered ring formation reaction including a novel compound (6) through a novel compound (8) and yielding a compound (D); and a deprotection for yielding CTX1B. Also disclosed are novel compounds (1) to (8) which are particularly useful for synthesis of CTX1B and can be used for the synthesis of a ciguatoxin analogue.
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:US-7183417-B2 优先权日:2004-04-09 标题:Simple stereocontrolled synthesis of salinosporamide A 发明人:COREY ELIAS J 权利人:HARVARD COLLEGE 摘要:A simple and effective stereocontrolled synthesis of salinosporamide A(1) n nhas been developed which follows the pathway outlined in the FIGURE. The process, the first total synthesis of salinosporamide A, is capable of providing the compound in substantial quantities for further biological studies. In addition to the method of Scheme I, the present invention also includes several novel synthetic intermediate compounds, several intermediate steps of the preferred synthetic process; and the uses of these compounds in the preparation of synthetic derivatives of the compound Salinosporamide A. Salinosporamide A is of special interest as a synthetic target because of its protein in vitro cytotoxic activity against many tumor cell lines (IC 50 values of 10 nM or less).
专利号:US-2004018598-A1 优先权日:2000-05-30 标题 :Bio-intermediates for use in the chemical synthesis of polyketides 发明人:SANTI DANIEL; ASHLEY GARY; MYLES DAVID C 摘要:The present invention relates to compounds made by a subset of modules from one or more polyketide synthase (“PKSâ€?) genes that are used as starting material in the chemical synthesis of novel molecules, particularly naturally occurring polyketides or derivatives thereof. The biologically derived intermediates (“bio-intermediatesâ€?) generally represent particularly difficult compounds to synthesize using traditional chemical approaches due to one or more stereocenters. In one aspect of the invention, an intermediate in the synthesis of epothilone is provided that feeds into the synthetic protocol of Danishefsky and co-workers. In another aspect of the invention, intermediates in the synthesis of discodermolide are provided that feed into the synthetic protocol of Smith and co-workers. By taking advantage of the inherent stereochemical specificity of biological processes, the syntheses of key intermediates and thus the overall syntheses of compounds like epothilone and discodermolide are greaty simplified.
专利号:WO-2020246902-A1 优先权日:2019-06-07 标 题 :An initiator of atrp radical polymerisation, a method of its synthesis, and a method of synthesis of low-dispersion polymer and copolymer using this initiator 发明人:MEGIEL ELÅ»BIETA; ROMAŃSKI JAN; FEDORCZUK MAGDALENA 权利人:UNIV WARSZAWSKI 摘要:An initiator of ATRP radical polymerisation having a functional group with a substituent active in polymerisation process, is characterised in that it is a bifunctional initiator containing at least two functional groups separated by a hydrocarbon moiety Y, where the first functional group has an active substituent X and the second functional group has a protecting group Z, which can be chemically modified with the same or a different substituent than the active substituent X present in the first functional group. A method of synthesis of 2-chloro-N-(2-hydroxyethyl)propionamide initiator, NCPAE, is characterised in that ethanolamine is subjected to an acylation reaction with 2-chloropropionyl chloride in presence of triethylamine (TEA), wherein the reaction is carried out under inert atmosphere at room temperature.
专利号:US-3992439-A 优先权日:1972-04-17 标 题:Synthesis of prostaglandins of the 'one'-series 发明人:SCHAAF THOMAS K; COREY ELIAS J 权利人:PFIZER 摘要:In the synthesis of prostaglandins of the 'one' -series an alteration in the conventional reaction sequence avoids side reactions and provides an improved synthesis via a series of novel intermediates. In this improved synthesis the side chain at the 8 position is attached to the five membered ring before the side chain at the 12 position is attached.
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