原甲酸三乙酯置于二异丁基氢化铝体系中,用 正己烷 作为反应溶剂,以76%的收率获得产物二乙氧基甲烷 参考文献:Volkov,A. A.; Zlot-Skii,S. S.; Kravets,E. Kh.,Journal Of General Chemistry Of The Ussr,1986,Vol. 56,# 12,P. 2400-2402 标题:Volkov,A. A.; Zlot-Skii,S. S.; Kravets,E. Kh.,Journal Of General Chemistry Of The Ussr,1986,Vol. 56,# 12,P. 2400-2402
专利号:WO-2025053792-A1 优先权日:2023-09-06 标题:Collective synthesis of phantomolin family through total synthesis of the sesquiterpene lactone molephantin 发明人:CHIBA SHUNSUKE; PATOURET REMI HENRI LOUIS; LI HOI YEUNG; LAI SOAK KUAN 权利人:UNIV NANYANG TECH 摘要:Disclosed herein are processes to generate an intermediate in the total synthesis of (+)- molephantin or a derivative thereof, and a total synthesis of (+)-molephantin or a derivative thereof. Also disclosed herein are methods of forming a compound of formula XIV and of forming a compound of formula XV, wherein compound of formula XIV and compound of formula XV are as defined in the description.
专利号:US-2006287520-A1 优先权日:2005-05-16 标 题 :Synthesis of salinosporamide A and analogues thereof 发明人:DANISHEFSKY SAMUEL J; ENDO ATSUSHI 权利人:DANISHEFSKY SAMUEL J; ENDO ATSUSHI 摘要:A novel synthesis of salinosporamide A is provided. Salinospoamide A as well as structurally related natural products, omuralide and lactacystin, have been shown to be proteasome inhibitors. Therefore, these compounds as well as analogues of these natural products may be useful in the treatment of proliferative diseases such as cancer, autoimmune diseases, diabetic retinopathy, etc. The invention provides for the synthesis of salinosporamide A as well as analogs thereof using a convenient point for derivatization of the bicyclic core. Pharmaceutical compositions and method of using the inventive compounds are also provided.
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-6028237-A 优先权日:1996-12-16 标题:Synthesis of cyclopropylacetylene 发明人:PARSONS JR RODNEY LAWRENCE 权利人:DU PONT PHARM CO 摘要:The present invention relates generally to novel methods for the synthesis of cyclopropylacetylene which is a reagent in the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one which is a useful human immunodeficiency virus (HIV) reverse transcriptase inhibitor.
专利号:US-5663467-A 优先权日:1995-01-23 标题:Synthesis of cyclopropylacetylene 发明人:THOMPSON ANDREW S; CORLEY EDWARD G; HUNTINGTON MARTHA 权利人:MERCK & CO INC 摘要:An improved synthesis of cyclopropylacetylene involving cyclization of 5-halo-1-pentyne in strong base is disclosed, and is useful for preparing compounds with a cyclopropylethynyl substituent, such as an intermediate for a highly potent HIV reverse transcriptase inhibitor or other pharmaceutically active compounds.
专利号:US-8742028-B2 优先权日:2009-05-06 标 题:Solid support for Fmoc-solid phase synthesis of peptide acids 发明人:SRIVASTAVA KRIPA S; DAVIS MATTHEW R 权利人:SRIVASTAVA KRIPA S; DAVIS MATTHEW R; MALLINCKRODT LLC 摘要:The present invention provides a solid support for Fmoc-solid phase synthesis of peptides. In particular, the solid supports of the invention may be utilized to produce peptide acids.