二甲氨基甲醇置于碘代三甲硅烷体系中,用 乙醚 作为反应溶剂,化学反应 0.5H,反应生成 N,N-二甲基亚甲基碘化胺 参考文献:The Synthesis Of Primary,Secondary And Tertiary Aminomethyltetrathiafulvalenes 标题:The Synthesis Of Primary,Secondary And Tertiary Aminomethyltetrathiafulvalenes 摘要:The Title Compounds Have Been Prepared In One Or Two Steps,Using Either Formyltetrathiafulvalene Or Tetrathiafulvalenyllithium As Starting Materials. DOI:10.1016/s0040-4020(01)88478-7
专利号:WO-2012047907-A9 优先权日:2010-10-04 标题 :Synthesis of c5-substituted tetracyclines, uses thereof, and intermediates thereto 发明人:MYERS ANDREW G; WRIGHT PETER M; HECKER EVAN 权利人:HARVARD COLLEGE; MYERS ANDREW G; WRIGHT PETER M; HECKER EVAN 摘要:The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides more efficient routes for preparing the enone intermediate and allows for a wide variety of substituents at position 5 of the tetracycline ring system.
专利号:WO-0140193-A1 优先权日:1999-12-03 标题:Method for the synthesis of pyrazolines 发明人:BOLDI ARMEN M 权利人:CHEMRX ADVANCED TECHNOLOGIES I; BOLDI ARMEN M 摘要:The present invention provides a method for the synthesis of compounds of Formula (I). Also claimed are novel intermediates and their methods of synthesis.
专利号:US-9688644-B2 优先权日:2009-04-30 标 题 :Synthesis of Tetracyclines and intermediates thereto 发明人:MYERS ANDREW G; KUMMER DAVID A; LI DERUN; HECKER EVAN; DION AMELIE; WRIGHT PETER M 权利人:HARVARD COLLEGE 摘要:The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides more efficient routes for preparing the enone intermediate and allows for substituents at positions 4a, 5, 5a, and 12a of the tetracycline ring system.
专利号:US-2002103381-A1 优先权日:2000-11-30 标 题 :Method for the synthesis of pyrazolines 发明人:BOLDI ARMEN M 摘要:The present invention provides a method for the synthesis of compounds of Formula I: n n n Also claimed are novel intermediates and their methods of synthesis.
专利号:US-7276637-B2 优先权日:2002-08-02 标题:Synthesis of cyclohexanone derivatives 发明人:BRANDS KAREL MARIE JOSEPH; DAVIES ANTONY JOHN; OAKLEY PAUL JOSEPH; SCOTT JEREMY PETER; SHAW DUNCAN EDWARD; TEALL MARTIN RICHARD 权利人:MERCK & CO INC 摘要:A novel process for preparing cyclohexanone derivatives of formula (I) n nis described. The products are useful as gamma secretase inhibitors, or as intermediates in the synthesis of other gamma secretase inhibitors.
专利号:US-10995093-B2 优先权日:2016-04-07 标 题 :Synthesis of 2′-fluoro-6′-methylene-carbocyclic adenosine (FMCA) and 2′-fluoro-6′methylene-carbocyclic guanosine (FMCG) 发明人:CHU CHUNG K; MULAMOOTTTIL VARUGHESE ALEXANDER; MISHRA RAM C; SINGH UMA SHARAN 权利人:UNIV GEORGIA 摘要:The invention provides a new convergent approach for the synthesis of 2′-fluoro-6′-methylene-carbocyclic adenosine (FMCA) and 2′-fluoro-6′-methylene-carbocyclic guanosine (FMCG) from a readily available starting material in eight steps. An efficient and practical methodology for stereospecific preparation of a versatile carbocyclic key intermediate, (1S,3R, 4R)-3-tert-butoxy-4-(tert-butoxymethyl)-2-fluoro-5-methylenecyclopentanol (compound 8 of scheme 1A or a) in only six (6) steps is also provided. Prodrugs of these compounds are also prepared.
[参考文献]: Masayuki Inoue, Et Al. Total Synthesis And Bioactivity Of An Unnatural Enantiomer Of Merrilactone A: Development Of An Enantioselective Desymmetrization Strategy. J Org Chem. 2007 Apr 13;72(8):3065-75.
合成参考文献
摘要:Zhang, F.-L.; Wang, Y.-F., Science of Synthesis, (2021) , 381.