专利号:WO-2009026961-A1 优先权日:2007-08-30 标 题:Processes for the preparation of pancratistatin and pancratistatin analogues 发明人:ALONSO ALONSO RICARDO; OZORES VITURRO LIDIA; CAGIDE FAGIN FERNANDO; ORTIZ LARA JUAN CARLOS 权利人:UNIV SANTIAGO COMPOSTELA; ALONSO ALONSO RICARDO; OZORES VITURRO LIDIA; CAGIDE FAGIN FERNANDO; ORTIZ LARA JUAN CARLOS 摘要:Processes for the preparation of pancratistatin and pancratistatin analogues. The key step is the reaction of a 1,3-dioxan-5-one and a nitroolefine in the presence of an amine. The process may take place in an enantioselective way when a chiral amine is used. Reduction processes then give new and advanced intermediates that are useful for the preparation of pancratistatin or selected pancratistatin analogues. The reported process also provides a method for the efficient synthesis of nitroenals, starting materials of the synthesis. Analogues of pancratistatin are also provided.
专利号:US-5569786-A 优先权日:1987-01-06 标 题 :Isolation, structural elucidation and synthesis of novel antineoplastic substances denominated 'combretastatins' 发明人:PETTIT GEORGE R; SINGH SHEO B 权利人:UNIV ARIZONA 摘要:New antineoplastic substances have been isolated, structurally elucidated and synthesized having a general structural formula of: (I) or H or OCH3; or R1R2 is -OCH2O-; R3 is H or OH; and R4 is OH or OCH3. These substances have been denominated 'combretastatin A-1, -A-2, -A-3, -B-1, -B-2, -B-3 and -B-4'. preparation containing the substances and methods of treating a host inflicted with a neoplastic growth with the preparation is described.
专利号:WO-0053313-A2 优先权日:1999-03-09 标 题:Lanthanide catalysts for synthesis of compounds and combinatorial libraries
专利号:US-5409953-A 优先权日:1987-01-06 标题:Isolation, structural elucidation and synthesis of novel antineoplastic substances denominated 'combretastatins'
专利号:US-2006160773-A1 优先权日:2003-07-18 标 题 :Combretastatin derivatives with cytotoxic action 发明人:GIANNINI GIUSEPPE; PISANO CLAUDIO; ALLOATTI DOMENICO; ROMAGNOLI ROMEO; SIMONI DANIELE 权利人:GIANNINI GIUSEPPE; PISANO CLAUDIO; ALLOATTI DOMENICO; ROMAGNOLI ROMEO; SIMONI DANIELE 摘要:The invention described herein relates to new combretastatin derivatives obtained by total synthesis and having the following general formula: n nin which the groups are as defined in the description here below. Said compounds, though chemically related to the structure of cis/trans-combretastatin, do not always bind tubulin, but nevertheless exhibit cytotoxic activity of interest in the oncological field as anticancer and/or antiangiogenic agents.