3,4-二氢-2H-吡喃置于titanium(III) Chloride Sodium Tetrahydroborate,18-冠醚-6,双氧水,Sodium Methylate体系中,化学反应生成3-羟基四氢吡喃 参考文献:Regio-And Stereo-Selectivities In The Titanium Complex Catalyzed Hydroboration Of Carbon-carbon Double Bonds In Various Unsaturated Compounds 标题:Regio-And Stereo-Selectivities In The Titanium Complex Catalyzed Hydroboration Of Carbon-carbon Double Bonds In Various Unsaturated Compounds 摘要:由ticl3和nabh4在thf中,在18-冠-6的存在下制备的钛配合物催化了烯烃,烯烃二烯和不饱和醚的碳-碳双键的氢硼化反应,生成的钠有机硼化合物可以通过h2O2/ch3Ona氧化转化为醇.该反应具有很高的区域选择性和立体选择性. Doi:10.1246/cl.1984.673
专利号:WO-9419366-A1 优先权日:1993-02-26 标题 :Chemical synthesis of squalamine 发明人:MORIARTY ROBERT M; GUO LIANG; TULADHAR SUDERSAN M 权利人:MAGAININ PHARMA 摘要:Methods for the chemical preparation or synthesis of the sterol antibiotic squalamine. Preferably, the preparation is by modifying the 3-position of a 3-oxo-7α-hydroxy-24z-ether protected alcohol group-5α-cholestane with a spermidino moiety to form a 3β-spermidino-7α-hydroxy-24z-ether protected group -5α-cholestane; deprotecting the 24-position of the 3β-spermidino-7α-hydroxy-24z-ether protected group-5α-cholestane to the free hydroxyl; and sulfating the 24-position of the 3β-spermidino-7α, 24-dihydroxy-5α-cholestane.
专利号:US-8487108-B2 优先权日:2005-11-14 标题 :Piperidinyl carbamate intermediates for the synthesis of aspartic protease inhibitors 发明人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T 权利人:BALDWIN JOHN J; CLAREMON DAVID A; TICE COLIN; CACATIAN SALVACION; DILLARD LAWRENCE W; ISHCHENKO ALEXEY V; YUAN JING; XU ZHENRONG; MCGEEHAN GERARD; SIMPSON ROBERT D; SINGH SURESH B; ZHAO WEI; FLAHERTY PATRICK T; VITAE PHARMACEUTICALS INC 摘要:The present invention is directed to aspartic protease inhibitors. Certain aspartic protease inhibitors of the invention can be represented by the following structural formula or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.
专利号:US-8338628-B2 优先权日:2007-08-28 标题 :Method of synthesizing alkylated bile acid derivatives 发明人:YU DONNA D; FORMAN BARRY M 权利人:YU DONNA D; FORMAN BARRY M; HOPE CITY 摘要:A novel, improved method of synthesizing alkylated bile acid derivatives is provided. Such derivatives include, but are not limited to the active, potent, and selective FXR receptor agonist such as 6-ECDCA and other CA, DCA and CDCA derivatives. The first step of the synthesis selectively oxidates CDCA, CD, or DCA related starting material. An efficient combined deprotonation, trapping, ethylation, deprotection and reduction system is used to produce the desired alkylated bile acid derivatives. This practical synthesis offers a simple and economical pathway suitable for a large-scale manufacturing of alkylated bile acid derivatives including, but not limited to, 6-ECDCA.
专利号:EP-3292130-B1 优先权日:2015-05-07 标题:Macrocyclization reactions and intermediates and other fragments useful in the synthesis of halichondrin macrolides
专利号:US-2018118755-A1 优先权日:2015-05-07 标题:Macrocyclization reactions and intermediates and other fragments useful in the synthesis of halichondrin macrolides
专利号:CN-117024469-A 优先权日:2015-05-07 标 题 :Can be used in macrocyclization reactions for the synthesis of halichondrin macrolides as well as intermediates and other fragments
摘要:Demchenko, A. V.; De Meo, C., Science of Synthesis Knowledge Updates, (2010) 3, 313. 摘要:Demchenko, A. V.; De Meo, C., Science of Synthesis Knowledge Updates, (2010) 3, 239. 摘要:Nakagawa, Y.; Tamura, M.; Tomishige, K., Science of Synthesis: Catalytic Reduction in Organic Synthesis, (2017) 1, 253.