📜异丙基三氯硅烷,乙基锂 以 四氢呋喃,乙醚 用作溶剂,化学反应 18.0H,反应生成二乙基异丙基氯硅烷 参考文献:Steroidal Silicon Side-Chain Analogs As Potential Antifertility Agents 标题:Steroidal Silicon Side-Chain Analogs As Potential Antifertility Agents 摘要:A Number Of Silicon-Substituted Analogues Of Ethynylestradiol That Exhibit Modified And Enhanced Biological Activities Have Been Synthesized. Particularly Noteworthy Are A Group Of [(Trialkylsilyl)Ethynyl]Estradiol Analogues That Exhibit High Antifertility Potency And Markedly Reduced Estrogenic Activity. The Best Compounds Synthesized Are 17 Alpha-[(Triethylsilyl)Ethynyl]Estradiol (5) And 17 Alpha-[(Tert-Butyldimethylsilyl)Ethynyl]Estradiol (33),Which Show A Separation Of Antifertility From Estrogenic Activity In The Rat. The Results Of Structure-Activity Studies Indicate A Good Correlation Between The Observed Biological Activities And The Calculated Van Der Waals Volumes Of The Three Variable Silicon Substituents. Doi:10.1021/jm00387A011
专利信息
专利号:US-7342003-B2 优先权日:2001-10-25 标 题 :Synthesis of 2-aralkyloxyadenosines, 2-alkoxyadenosines, and their analogs 发明人:MOORMAN ALLAN R; SCANNELL MICHAEL; BALASUBRAMANIAN THIAGARAJAN; OUTCALT RUSSELL; LEUNG EDWARD 权利人:KING PHARMACEUTICALS RES & DEV 摘要:Provided is a method for the synthesis of an aralkyloxyadenosine or an alkoxyadenosine. The method includes protecting the hydroxyl sugar groups with a protecting group to produce a protected halogenated adenosine. The protected halogenated adenosine is alkoxylated, and the hydroxyl sugar groups of the protected halogenated adenosine are deprotected to provide the aralkyloxyadenosine or alkoxyadenosine.
专利号:US-7884128-B2 优先权日:2005-10-13 标题:Process for total synthesis of pladienolide B and pladienolide D 发明人:KANADA REGINA MIKIE; ITO DAISUKE; SAKAI TAKASHI; ASAI NAOKI; KOTAKE YOSHIHIKO; NIIJIMA JUN 权利人:EISAI R&D MAN CO LTD 摘要:Process for producing compound of Formula: n nwherein P 2 , P 3 and R 2 are the same as defined below, characterized by comprising reacting a compound represented by Formula (7):n n nwherein P 3 means a protecting group for hydroxy group; and Het means a 1-phenyl-1H-tetrazol-5-yl group, with a compound represented by Formula (8):n n nwherein P 2 means a protecting group for hydroxy group; and R 2 means a phenyl group which may be substituted, in the presence of a base.
专利号:US-12415828-B2 优先权日:2014-08-22 标题:Modified oligonucleotides and methods for their synthesis 发明人:STETSENKO DMITRY; KUPRYUSHKIN MAXIM; PYSHNYI DMITRII 权利人:NOOGEN LLC 摘要:Modified oligonucleotides that contain one or more of the phosphate groups substituted at phosphorus and methods for their synthesis are disclosed.
专利号:US-2006135466-A1 优先权日:2001-10-25 标题 :Synthesis of 2-aralkyloxyadenosines, 2-alkoxyadenosines, and their analogs
专利号:US-4684724-A 优先权日:1981-12-25 标题:4-Cyano-2-azetidinones and production thereof 发明人:OCHIAI MICHIHIKO; KISHIMOTO SHOJI; MATSUO TAISUKE 权利人:TAKEDA CHEMICAL INDUSTRIES LTD 摘要:4-Cyano-2-azetidinone derivatives represented by the formula ##STR1## wherein R 1 is an amino group which may be acylated or protected, X is a hydrogen atom or a methoxy group and W is a hydrogen atom or a sulfo group, and methods of producing the same, for example, as represented by ##STR2## wherein R 2 is an acylated or protected amino group, Y is a halogen atom or a group having the formula --OCOR 3 , --SCOR 3 or --S(O) n --R 3 (R 3 being a hydrocarbyl group and n an integer 1 or 2), R 4 is an amino group which may be acylated or protected and X is as defined above. Compounds [I] are useful as advantageous intermediates for the synthesis of optically active 4-substituted-2-azetidinone derivatives, and, when W=SO 3 H, [I] are also useful as antimicrobial agents and as beta-lactamase inhibitors.
专利号:US-2008021226-A1 优先权日:2005-10-13 标题:Process for total synthesis of pladienolide B and pladienolide D
参考标题:Total Synthesis Of The Macrolide Antibiotic Cytovaricin 作者:David A. Evans,Stephen W. Kaldor,Todd K. Jones,Jon Clardy,Thomas J. Stout |发布日期:1990.9 摘要:A Convergent Asymmetric Synthesis Of The Antinoeplastic Macrolide Antibiotic Cytovaricin Has Been Achieved Through The Synthesis And Coupling Of The Illustrated Spiroketal And Polyol Glycoside Subunits. All Absolute Steroechemical Relationships Within The Target Structure Were Ultimately Controlled By The Use Of Asymmetric Aldol, Alkylation, Or Epoxidation Methodology. Union Of The Two Subnits Was