专利号:US-8829184-B2 优先权日:2010-04-15 标题:Intermediates useful for the synthesis of pyrrolobenzodiazepines 发明人:HOWARD PHILIP WILSON; MASTERSON LUKE; TIBERGHIEN ARNAUD 权利人:HOWARD PHILIP WILSON; MASTERSON LUKE; TIBERGHIEN ARNAUD; SPIROGEN SARL 摘要:A compound of formula (I): which is substantially free of any of the corresponding compound of formula (IB): methods of making such compounds, and the further transformation of such compounds.
专利号:US-9670234-B2 优先权日:2014-07-10 标题 :Metal-catalyzed asymmetric 1,4-conjugate addition of vinylboron compounds to 2-substituted-4-oxy-cyclopent-2-en-1-ones yielding prostaglandins and prostaglandin analogs 发明人:HENSCHKE JULIAN PAUL; WU PING-YU; WU HSYUEH-LIANG; WEN WEN-HSIEN 权利人:SCINOPHARM TAIWAN LTD 摘要:This invention provides a novel method for the preparation of 2,3-disubstituted -4-oxy-cyclopentan1-one compounds that are useful for the synthesis of prostaglandins and prostaglandin analogs of industrial relevance. The method comprises the metal-catalyzed asymmetric 1,4-conjugate addition of vinylboron compounds to 2-substituted -4-oxy-cyclopent-2-en-1-ones. This method relies on the use of less toxic, easily-handled reagents, and can be performed under milder conditions than offered by some conventional methods, affording 2,3-disubstituted-4-oxy-cyclopentan-1-one compounds enantio- and diastereoselectively, which are precursors to the said prostaglandin and prostaglandin analogs, in high yield.
专利号:US-2013035484-A1 优先权日:2010-04-15 标 题:Intermediates useful for the synthesis of pyrrolobenzodiazepines
专利号:WO-2011128650-A1 优先权日:2010-04-15 标 题:Intermediates useful for the synthesis of pyrrolobenzodiazepines
专利号:JP-2013523875-A 优先权日:2010-04-15 标题:Useful intermediates for the synthesis of pyrrolobenzodiazepines.
专利号:EP-2558445-A1 优先权日:2010-04-15 标 题:Intermediates useful for the synthesis of pyrrolobenzodiazepines
参考文献:10.1021/jo800545r 摘要:Ghidu VP, Wang J, Wu B, Liu Q, Jacobs A, Marnett LJ, Sulikowski GA. Synthesis and evaluation of the cytotoxicity of apoptolidinones A and D. J Org Chem. 2008 Jul 04;73(13):4949–55.