专利号:US-8461384-B2 优先权日:2006-12-11 标 题 :Preparation of amides from an acid and amine for intermediates in the synthesis of morphinans 发明人:WANG PETER X; MOSER FRANK W; GROTE CHRISTOPHER W; CANTRELL GARY L 权利人:WANG PETER X; MOSER FRANK W; GROTE CHRISTOPHER W; CANTRELL GARY L; MALLINCKRODT LLC 摘要:The present invention is directed to processes for the synthesis of morphinans. In particular, a process for coupling a carboxylic acid compound with an amine compound to form an amide product that can then be isolated or the crude amide product can be cyclized to form a 3,4-dihydroisoquinoline. In one embodiment, the carboxylic acid contains a phenol moiety protected with a labile protecting group. The protected phenol reduces reaction times, simplifies work-up of the product, and reduces the amount of cyclizing agent, POCl 3 that is necessary to form the 3,4-dihydroisoquinoline.
专利号:US-2009306400-A1 优先权日:2006-03-27 标 题:Convergent process for the synthesis of taxane derivatives. 发明人:HENRI JOHN T; MCCHESNEY JAMES D; VENKATARAMAN SYLESH K; LAMB RODGER L; FOSTER JONATHAN E; SUMNER CHRISTIAN M; YE SHANGPING 权利人:HENRI JOHN T; MCCHESNEY JAMES D; VENKATARAMAN SYLESH K; LAMB RODGER L; FOSTER JONATHAN E; SUMNER CHRISTIAN M; YE SHANGPING 摘要:The present invention is broadly directed to novel compounds useful for the synthesis of biologically active compounds, including taxane derivatives, and convergent processes for the preparation of these taxane derivatives and their intermediates.
专利号:US-5948693-A 优先权日:1994-09-01 标题:Solid phase synthesis of immunosuppressive agents 发明人:RICH DANIEL H; RAMAN PRAKASH; ANGELL YVONNE M 权利人:WISCONSIN ALUMNI RES FOUND 摘要:The present invention relates generally to cyclosporin analogs, and more paritcularly to methods for the solid-phase synthesis and on-resin cyclization of cyclosporin analogs. Methods are described for the on-resin cyclization of sterically hindered compounds synthesized through solid phase synthesis techniques. The methods utilize solvent, temperature, and washing conditions that allow the efficient on-resin cyclization of compounds like analogs of cyclosporin A.
专利号:WO-9845231-A1 优先权日:1997-04-09 标题:Supports for solid phase synthesis 发明人:SHAO HUI; CASTELHANO ARLINDO L 权利人:CADUS PHARMACEUTICAL CORP 摘要:Supports for solid-phase synthesis are disclosed. The supports include a phenol or thiophenol linker moiety. A substrate compound can be immobilized to the support through the linker moiety. The supports are suitable for combinatorial synthesis, including synthesis of combinatorial libraries.
专利号:US-5866700-A 优先权日:1993-12-17 标 题:Solid-phase synthesis of oligoribonucleotides 发明人:PFLEIDERER WOLFGANG; SCHNELL RALF; MATYSIAK STEPHAN 权利人:HOECHST AG 摘要:A process for the preparation of oligoribonucleotides of the formula in which n, L, BB, W, T, Y', U, C1 and C2 are as defined in the description, by solid-phase synthesis is described, as are intermediates of the oligoribonucleotides.
专利号:US-9403841-B2 优先权日:2012-01-25 标题:Phragamalin limonoids for the treatment of sexual dysfunction 发明人:WIKBERG JARL; JIRGENSONS AIGARS; LIEPINSH EDVARDS 权利人:DICOTYLEDON AB 摘要:The present invention relates to novel chemical compounds, to methods for synthesis of such compounds, and to the use of these novel compounds in the synthesis of other chemical compounds that, inter alia, may be used in the treatment of sexual dysfunction, and for eliciting enhancing effects on sexual behavior. The invention also relates to remarkable biological properties of the novel compounds in their capacity of inducing aggressive behavior.
参考标题:Synthesis Of Ortho-Phenolic Sulfilimines Via An Intermolecular Sulfur Atom Transfer Cascade Reaction 作者:Feng Xiong,Yingying Zuo,Yinan Song,Linxing Zhang,Xinhao Zhang,Shaojian Xu,Yan Ren |发布日期:2020.5.15 摘要:To Expand The Toolbox For The Synthesis Of Ortho-Phenolic Sulfilimines, Sigmatropic Rearrangements Were Introduced To The Field Of Sulfilimine Chemistry. Herein We Report A N-H Sulfenylation/[2,3]-Sigmatropic Rearrangement Cascade Reaction. This Mild Reaction Enables Commercially Available Thiols To Serve As The Sulfenylation Reagent And Generates Water As The Sole Byproduct. Moreover, The Reaction
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