2-噻吩甲醛置于sodium Hydride,二异丁基氢化铝体系中,用 四氢呋喃,甲苯 用作溶剂,化学反应 4.0H,反应生成3-(2-噻吩)丙烯酸 参考文献:手性环戊二烯基铱(III)配合物可促进对映选择性环化异构化,生成熔融环丙烷 标题:手性环戊二烯基铱(III)配合物可促进对映选择性环化异构化,生成熔融环丙烷 摘要:环戊二烯基(cp)基团是许多在催化中应用的过渡金属配合物的重要配体.手性环戊二烯基配体(cp X)的可用性落后于其他配体类别,因此妨碍了对映选择性过程的研究.我们报告了配备手性cp支架的手性cp X Ir Iii复合物的库.强大的络合程序可为cp X Ir Iii络合物可靠地提供可调节的抗衡离子.在概念验证的应用中,含碘化物对烯炔的环异构化反应具有很高的选择性.脱氢哌啶稠合的环丙烷产物以非常好的收率和对映选择性形成. Doi:10.1002/anie.201506483
专利号:US-7109377-B2 优先权日:1996-10-16 标 题:Synthesis of combinatorial libraries of compounds reminiscent of natural products 发明人:SCHREIBER STUART L; SHAIR MATTHEW D; TAN DEREK S; FOLEY MICHAEL A; STOCKWELL BRENT R 权利人:HARVARD COLLEGE 摘要:The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis. Furthermore, the present invention provides methods and kits for determining one or more biological activities of members of the inventive libraries. Additionally, the present invention provides pharmaceutical compositions containing one or more library members.
专利号:US-5981239-A 优先权日:1997-09-24 标 题 :Synthesis of optically active phenylalanine analogs using Rhodotorula graminis 发明人:LIU WEIGUO 权利人:GREAT LAKES CHEMICAL CORP 摘要:A biocatalytic process to produce optically active phenylalanine analogs from arylacrylic acids is disclosed in which Rhodotorula graminis yeast containing phenylalanine ammonia-lyase introduces a molecule of ammonia stereoselectively onto the double bond of a 3-substituted acrylic acid. The substituent at the 3-position of the 3-substituted acrylic acid includes, for example, aromatic rings such as substituted phenyl groups, five member aromatic heterocyclics, and six member aromatic heterocyclics.
专利号:US-4563537-A 优先权日:1982-09-27 标题:Synthesis of thiophene-containing prostaglandin endoperoxide apparatus 发明人:LAROCK RICHARD C 权利人:UNIV IOWA STATE RES FOUND INC 摘要:New organopalladium reactions involving the addition of thienylpalladium compounds to strained bicyclic alkenes, and subsequent chain extension reactions employing the chemistry of organopalladium compounds are disclosed. By these techniques a large number of bicyclic prostaglandin analogs are prepared, which are useful as inhibitors of arachidonic acid induced blood platelet aggregation, and are specific inhibitors of thromboxane synthetase.
专利号:US-4520207-A 优先权日:1982-09-27 标 题:Synthesis of thiophene-containing prostaglandin endoperoxide analogs 发明人:LAROCK RICHARD C 权利人:UNIV IOWA STATE RES FOUND INC 摘要:New organopalladium reactions involving the addition of thienylpalladium compounds to strained bicyclic alkenes, and subsequent chain extension reactions employing the chemistry of organopalladium compounds are disclosed. By these techniques a large number of bicyclic prostaglandin analogs are prepared, which are useful as inhibitors of arachidonic acid induced blood platelet aggregation, and are specific inhibitors of thromboxane synthetase.
专利号:US-9085605-B2 优先权日:2010-05-27 标 题:Chemical synthesis and anti-tumor and anti-metastatic effects of dual functional conjugate 发明人:LIU GANG; ZHAO NAN; MA YAO 权利人:LIU GANG; ZHAO NAN; MA YAO; SHENZHEN SALUBRIS PHARM CO LTD 摘要:The present invention discloses chemical synthesis, anti-tumor and anti-metastatic effects of a dual functional conjugate as shown by formula I. Specifically, paclitaxel or docetaxol is linked with muramyl dipeptide derivative to form a conjugate, thus dual anti-tumor and anti-metastatic effects are achieved by combination of chemotherapy and immunotherapy. The present invention also discloses that paclitaxel or docetaxol and muramyl dipeptide derivative conjugate is synthesized by combination of solid-phase and solution-phase synthesis, and said conjugate can be used in manufacture of anti-tumor medicaments as proved by reliable bioassays.
专利号:US-2003082830-A1 优先权日:1996-10-16 标 题:Synthesis of combinatorial libraries of compounds reminiscent of natural products
摘要:Silva, V. L. M.; Pinto, D. C. G. A.; Santos, C. M. M.; Rocha, D. H. A., Science of Synthesis Knowledge Updates, (2022) 3, 201. 摘要:Huy, P.; Czekelius, C., Science of Synthesis Knowledge Updates, (2019) 2, 129. 摘要:Kawęcki, R., Science of Synthesis Knowledge Updates, (2018) 4, 281. 摘要:Vashchenko, B. V.; Grygorenko, O. O., Science of Synthesis Knowledge Updates, (2021) 3, 399. 摘要:Vashchenko, B. V.; Grygorenko, O. O., Science of Synthesis Knowledge Updates, (2021) 3, 329.