专利号:US-5760237-A 优先权日:1995-08-25 标 题 :Synthesis of l-azatyrosine using pseudoephedrine as a chiral auxiliary 发明人:MYERS ANDREW G 权利人:CALIFORNIA INST OF TECHN 摘要:A practical synthesis of the potential chemotherapeutic agent L-azatyrosine is described. The key step involved the alkylation of (R,R)-(-)-pseudoephedrine glycinamide with 5-benzenesulfonyloxy-2-iodomethylpyridine and proceeded in 70-95% yield and 89-95% de. Simultaneous hydrolysis of the auxiliary and the benzenesulfonate protecting group afforded L-azatyrosine of ≧99% ee in 73% yield on multigram scale (recovery yield of (R,R)-(-)-pseudoephedrine: 90%).
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-2019047933-A1 优先权日:2016-03-15 标 题:Process for the synthesis of (2e, 4e, 6z, 8e)-8-(3,4-dihydronaphthalen-1(2h)-ylidene)-3,7-dimethylocta-2, 4, 6-trienoic acid 发明人:ABEL ULRICH; RÉPÃ?SI JÓZSEF; Szabó András; SZÜCSNÉ CSERÉPI STEFÃ?NIA; Bor Ã?dám 权利人:ABEL ULRICH; REPASI JOZSEF; SZABO ANDRAS; SZUECSNE CSEREPI STEFANIA; BOR ADAM; BRICKELL BIOTECH INC 摘要:This invention relates to a novel method for the synthesis of (2E,4E,6Z,8E)-8-(3,4-dihydronaphthalen-1(2H)-ylidene)-3,7-dimethylocta-2,4,6-trienoic acid. In particular, the invention relates to several improvements in several individual steps of the multi-step synthesis scheme
专利号:WO-2022256490-A9 优先权日:2021-06-03 标题:Improved synthesis of phosphoramidates for the treatment of hepatitis b virus 发明人:LOCKWOOD MARK 权利人:ANTIOS THERAPEUTICS INC 摘要:The synthesis of phosphoramidate prodrugs useful in the treatment of viral infections is disclosed. Specifically, an improved synthesis of phosphoramidate nucleotides useful in the treatment of Hepatitis B virus is disclosed.
专利号:US-11891351-B2 优先权日:2020-03-20 标 题 :Synthesis of capsaicin derivatives 发明人:LAGER ERIK 权利人:AXICHEM AS 摘要:The present invention relates to the synthesis of capsaicin derivatives, specifically to the synthesis of 6-heptyne derivatives of capsaicin.
摘要:Koo, S., Science of Synthesis, (2010) 45, 1406. 摘要:Abell, A. D.; Edmonds, M. K., Science of Synthesis, (2009) 46, 44. 摘要:Griesbeck, A. G.; Soldevilla, A., Science of Synthesis, (2008) 43, 376. 摘要:Ito, S.; Morita, N., Science of Synthesis, (2010) 45, 470. 摘要:Ohno, H.; Tomioka, K., Science of Synthesis, (2008) 44, 81.