合成目标产物 3-Methyl Butynol 主要起始原料 Acetone And Acetylene
(文献来源)合成步骤主要原料 Acetone 和 Acetylene
在 三乙烯二胺体系中,用 苯 用作溶剂,化学反应 2.0H,反应生成2-甲基-3-丁炔-2-醇 参考文献:Organoselenium Chemistry. Formation Of Acetylenes And Allenes By Syn Elimination Of Vinyl Selenoxides 标题:Organoselenium Chemistry. Formation Of Acetylenes And Allenes By Syn Elimination Of Vinyl Selenoxides 摘要: Doi:10.1021/ja00538A072
专利号:WO-2009104605-A1 优先权日:2008-02-18 标 题 :Novel intermediate for synthesis of ascofranone having various physiological activities, and novel shortened total synthesis method for ascofranone using the same 发明人:SAIMOTO HIROYUKI; HAGA YASUSHI 权利人:ARIGEN PHARMACEUTICALS INC; SAIMOTO HIROYUKI; HAGA YASUSHI 摘要:In the synthesis of ascofranone, a compound represented by formula (III), (IV), (V) or (VII) or an optical isomer thereof is used as an intermediate for the synthesis. [In the formulae, R 1 and R 2 independently represent a hydrogen atom, a C 1-7 alkyl group, a phenoxyalkyl group having a halogen atom on a carbon atom in a benzene ring therein, or a phenyl group having a C 1-7 alkoxy group or a C 1-7 alkoxycarbonyl group on a carbon atom in a benzene ring therein; and X represents a halogen atom or a group R 5 SO 3 (wherein R 5 represents a C 1-7 alkyl group or a phenyl group having a C 1-7 alkyl group on a carbon atom in a benzene ring therein).] By using the compound, it becomes possible to reduce the number of steps required for the total synthesis of ascofranone to 7 or 8 from 12 which is a number of the steps required for the conventional ascofranone total synthesis processes.
专利号:WO-2018019549-A1 优先权日:2016-07-28 标 题:Dioxolanone intermediate useful in the synthesis of homoharringtonine 发明人:ALLEGRINI PIETRO; CATTANEO CRISTIAN; CICERI DANIELE; GAMBINI ANDREA; PETERLONGO FEDERICO; CERISOLI LUCIA; LOMBARDO MARCO 权利人:INDENA SPA 摘要:The invention discloses 2-((2R,4R)-4-(4-(benzyloxy)-4-methylpent-2-yn-1-yl)-2-(tert-butyl)-5-oxo-1,3-dioxolan-4-yl)acetic acid of formula (XIX), a process for its preparation and processes for its conversion into enantiomerically pure (R)-2-(2-methoxy-2-oxoethyl)-6,6-dimethyltetrahydro-2H-pyran-2-carboxylic acid of formula (I), a molecule useful for the synthesis of Homoharringtonine.
专利号:US-12037623-B2 优先权日:2018-07-09 标 题 :Enzymatic synthesis of 4′-ethynyl nucleoside analogs 发明人:HUFFMAN MARK A; FRYSZKOWSKA ANNA; KOLEV JOSHUA N; DEVINE PAUL N; CAMPOS KEVIN R; TRUPPO MATTHEW; NAWRAT CHRISTOPHER C 权利人:MERCK SHARP & DOHME; MERCK SHARP & DOHME LLC 摘要:The present invention relates to an enzymatic synthesis of 4′-ethynyl-2′-deoxy nucleosides and analogs thereof, for example EFdA, that eliminates the use of protecting groups on the intermediates, improves the stereoselectivity of glycosylation and reduces the number of process steps needed to make said compounds. It also relates to the novel intermediates employed in the process.
专利号:US-4310467-A 优先权日:1980-10-22 标题:Process and intermediates for the synthesis of vitamin D3 metabolites 发明人:BATCHO ANDREW D; BERGER JR DONALD E; USKOKOVIC MILAN R 权利人:HOFFMANN LA ROCHE 摘要:The present disclosure is directed to a process and intermediates for the synthesis of Vitamin D 3 metabolites such as 1,25-dihydroxycholecalciferol, 25-hydroxycholecalciferol and 24R,25-dihydroxycholecalciferol from 17-keto steroids via intermediates having the natural steroid configuration at the 20-position. These novel intermediates are prepared from 17-keto steroids by reaction with ethyltriphenylphosphonium halides followed by reaction with formaldehyde to form comounds having the natural steroid configuration at the 20-position and which are suitable substrates for the preparation of the aforementioned Vitamin D 3 metabolites.
专利号:US-4056573-A 优先权日:1975-04-24 标题:Synthesis of acyclic, terpene alcohols 发明人:CLOSE RALPH E; DERFER JOHN M 权利人:SCM CORP 摘要:Shown is a process for the synthesis of acyclic, terpene alcohols, such as 3,7-dimethyloctan-1-o1 and 7-substituted hydroxy or ethoxy derivatives thereof, wherein 3-methylbut-1-yn or the 3-substituted hydroxy or ether derivative thereof is coupled with a C5 coupling reagent having the configuration X being a leaving group such as chloride, bromide, iodide, tosylate and mesylate; R being or OR', R' being a lower alkyl up to 5 carbon atoms, phenyl, substituted phenyl up to 10 carbon atoms, cycloalkyl or aralkyl up to 10 carbon atoms, followed by hydrogenation and saponification or deetherification.
专利号:US-8759508-B2 优先权日:2007-05-18 标 题 :Chromophoric silyl protecting groups and their use in the chemical synthesis of oligonucleotides 发明人:DELANEY MICHAEL OREN 权利人:DELANEY MICHAEL OREN; GE HEALTHCARE DHARMACON INC 摘要:The compounds are of class of chromophoric 1,2,3-triazolyl equipped silyl linking groups that are useful in the chemical synthesis of RNA. An example of a nucleoside comprising this group is
参考文献:10.1021/ja204557m 摘要:Crespo-Quesada M, Yarulin A, Jin M, Xia Y, Kiwi-Minsker L. Structure sensitivity of alkynol hydrogenation on shape- and size-controlled palladium nanocrystals: which sites are most active and selective J Am Chem Soc. 2011 Aug 17;133(32):12787–94. doi: 10.1021/ja204557m. 参考文献:10.1002/chem.201101166 摘要:Fjermestad T, Pericàs MA, Maseras F. A Computational Study on the Role of Chiral N‐Oxides in Enantioselective Pauson–Khand Reactions. Chemistry A European J. 2011 Jul 19;17(36):10050–7. doi: 10.1002/chem.201101166.