📜在 二苯基甲烷体系中,用 四氢呋喃 用作溶剂,化学反应生成2-三甲基硅基-1,3-二噻吩 参考文献:Carbon Acidity. 77. Ion Pair Carbon Acidities Of Some Silanes In Tetrahydrofuran 标题:Carbon Acidity. 77. Ion Pair Carbon Acidities Of Some Silanes In Tetrahydrofuran 摘要:The Relative Solvent-Separated Ion Pair (Ssip) Lithium Acidity (Pk(Li)/thf) And Contact Ion Pair (Cip) Cesium Acidity (Pk(Cs/thf)) Were Obtained For 9-Fluorenyltrimethylsilane (1) (21.3,21.6,Respectively) And 9-Fluorenyl-Tert-Butyldimethylsilane (2) (20.3,20.6,Respectively) In Thf. Values For Pk(Cs/thf) Were Determined At 25-Degrees-C For (P-Biphenylylmethyl)-Tert-Butyldimethylsilane (3),35.4,Benzyltrimethylsilane (4),37.5,Alpha,Alpha-Bis(Trimethylsilyl)Toluene (5),34.1,2-(Trimethylsilyl)-1,3-Dithiane (6),33.5,(Trimethylsilyl)Acetonitrile (7),28.8,And Tris(Trimethylsilyl)Methane (8),36.8. Some Thermodynamic Parameters Were Determined By Measurements At Other Temperatures,And Some Ionic Acidities (Pk(Fi)) Were Determined By Conductivity Studies. Carbanion Stabilization By These Silyl Substituents Varies From About 1 To Over 3 Pk Units In Different Systems. 9,9-Bis(Trimethylsilyl)Fluorene (9) Was Found To Undergo Silyl Transfer On Treatment With Various Carbanions,But This Reaction Is Slower Than Proton Transfer. Doi:10.1021/jo00059A031
专利号:US-8883846-B2 优先权日:2010-02-15 标题:Synthesis of bicyclic compounds and method for their use as therapeutic agents 发明人:WULFF JEREMY E; BRANT MICHAEL G; MASON JEREMY W; BROMBA CALEB M; BOULANGER MARTIN J 权利人:WULFF JEREMY E; BRANT MICHAEL G; MASON JEREMY W; BROMBA CALEB M; BOULANGER MARTIN J; UVIC INDUSTRY PARTNERSHIPS INC 摘要:Disclosed embodiments concern the synthesis and use of therapeutic compounds that for treating emerging flu strains and minimizing resistance to such strains. Methods for making the disclosed compounds concern using a base-mediated addition/cyclization sequence followed by functional group manipulation to develop functionalized compounds that can target neuraminidase, which makes them ideal candidates for treating influenza. Pharmaceutical compositions comprising the therapeutic compounds and biologically-acceptable materials are also described. Methods of inhibiting neuraminidase in subjects that are suspected of containing neuraminidase are also described. The use of metabolites of the disclosed compounds can also be used in diagnostic assays for therapeutic dosing of the disclosed compounds.
专利号:US-4383946-A 优先权日:1980-03-27 标题:Process for the preparation of 1-carbapenems and intermediates via silyl-substituted dithioacetals 发明人:CHRISTENSEN BURTON G; RATCLIFFE RONALD W; SALZMANN THOMAS N 权利人:MERCK & CO INC 摘要:Disclosed is a process for the total synthesis of 1-carbapenem antibiotics (I) from L-aspartic acid via central intermediates II and III: I II III wherein R is hydrogen, a pharmaceutically acceptable ester moiety or salt cation, or a readily removable blocking group; R6, R7 and R8 are, inter alia, independently selected from the group consisting of hydrogen, alkyl, alkenyl, aryl and aralkyl; R1'and Re are hydrogen, or a readily removable protecting group; Ra, Rb and Rc are selected from alkyl, aryl or aralkyl.
专利号:US-4610820-A 优先权日:1979-07-23 标 题:Process for the preparation of thienamycin and intermediates 发明人:CHRISTENSEN BURTON G; RATCLIFFE RONALD W; SALZMANN THOMAS N 权利人:MERCK & CO INC 摘要:In a process for the total synthesis of thienamycin from L-aspartic acid via intermediate III: ##STR1## R=H, blocking group or salt cation there is disclosed a process for preparing III via ##STR2## wherein R is a protecting group.
专利号:EP-0026816-B1 优先权日:1979-07-23 标题:Intermediates for the preparation of thienamycin and process for preparing intermediates 摘要:In a process for the total synthesis of thienamycin from L-aspartic acid via intermediate III: R = H, blocking group or salt cation there is disclosed a process for preparing III via wherein R is a protecting group.
专利号:US-6387893-B1 优先权日:1999-09-30 标题 :Spirotricyclic substituted azacycloalkane derivatives and uses thereof 发明人:EVANS BEN E; HOFFMAN JACOB M; GILBERT KEVIN F; RITTLE KENNETH E 权利人:MERCK & CO INC 摘要:Spirotricyclic azacycloalkyl compounds and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds is also described. One application of these compounds, which are alpha 1a adrenergic receptor antagonists, is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.
专利号:US-6326372-B1 优先权日:1999-09-30 标 题:Lactam and cyclic urea derivatives useful as alpha 1a adrenoceptor antagonists 发明人:EVANS BEN E; GILBERT KEVIN F 权利人:MERCK & CO INC 摘要:Lactam and cyclic urea derivatives and their pharmaceutically acceptable salts are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are typically selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.
[参考文献]: Amos B Smith Rd, Et Al. Multicomponent Linchpin Couplings. Reaction Of Dithiane Anions With Terminal Epoxides, Epichlorohydrin, And Vinyl Epoxides: Efficient, Rapid, And Stereocontrolled Assembly Of Advanced Fragments For Complex Molecule Synthesis. J Am Chem Soc. 2003 Nov 26;125(47):14435-45.
合成参考文献
摘要:Molander, G. A.; Beaumard, F., Science of Synthesis Knowledge Updates, (2013) 3, 119. 摘要:Nahm Garrett, M.; Johnson, J. S., Science of Synthesis Knowledge Updates, (2012) 2, 10. 摘要:Ishii, A., Science of Synthesis Knowledge Updates, (2016) 2, 354. 摘要:Saikawa, Y.; Nakata, M., Science of Synthesis Knowledge Updates, (2018) 3, 374. 摘要:Saikawa, Y.; Nakata, M., Science of Synthesis Knowledge Updates, (2018) 3, 378.