专利号:US-2023312617-A1 优先权日:2020-07-25 标题 :Process for synthesis of organosilicon compounds from halosilanes 发明人:DOLAI SUKANTA; BHAT SHREEDHAR; TARAFDAR GOURAV 权利人:MOMENTIVE PERFORMANCE MAT INC 摘要:A process for synthesis of an organosilicon compound is provided herein. Also, novel organosilicon compounds prepared by the present process is provided herein. The process comprises the reaction of a halosilane with an organofunctional alkyl halide in the presence of a metal catalyst, a promoter, and an optional co-catalyst. The process provides an efficient synthetic route to produce organosilicon compounds. The process also allows synthesis of organosilicon compounds with a plurality of different functional groups.
专利号:US-2025026768-A1 优先权日:2023-06-30 标题:Method for the synthesis of axially chiral organoboron compounds 发明人:PING YIFAN; CHE CHI-MING 权利人:LABORATORY FOR SYNTHETIC CHEMISTRY AND CHEMICAL BIOLOGY LTD 摘要:A highly efficient and atroposelective Rh-catalyzed [2+2+2] cycloaddition for the synthesis of axially chiral aryboron compounds is developed. The reactions of diynes and alkynylborons smoothly occur in an atom-economical manner, affording a variety of C—B atropisomers in excellent yields and enantioselectivities. The protocol features mild conditions, broad substrate scope, and good functional tolerance. The obtained C—B atropisomers show powerful synthetic applications in terms of producing novel chiral phosphine ligands.
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-5698741-A 优先权日:1995-05-25 标题 :Asymmetric synthesis of (-)6-chloro-4-cyclopropyl-ethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one 发明人:THOMPSON ANDREW S; CORLEY EDWARD G; GRABOWSKI EDWARD J J; YASUDA NOBUYOSHI 权利人:MERCK & CO INC 摘要:An improved synthesis of a highly potent HIV reverse transcription inhibitor is disclosed, involving an acetylide and a trifluoromethyl ketone which produces a chiral product in the presence of a chiral amino alcohol.
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:WO-9804535-A1 优先权日:1996-07-26 标 题 :A practical synthesis of benzoxazinones useful as hiv reverse transcriptase inhibitors 发明人:PIERCE MICHAEL ERNEST; RADESCA LILIAN ALICIA 权利人:DU PONT MERCK PHARMA 摘要:The present invention describes novel methods for the synthesis of benzoxazinone compounds which are useful as human immunodeficiency virus (HIV) reverse transcriptase inhibitors. The benzoxazinone of formula (VI-a) is particularly effective in the treatment of HIV.
[参考文献]: Xiangbing Qi, Et Al. Copper-Promoted Cycloaddition Of Diazocarbonyl Compounds And Acetylides. Angew Chem Int Ed Engl. 2007;46(18):3242-4.
合成参考文献
摘要:Tobe, Y.; Takeda, T., Science of Synthesis, (2010) 45, 1336. 摘要:de Meijere, A.; Kozhushkov, S. I., Science of Synthesis, (2009) 48, 495. 摘要:Amatore, M.; Aubert, C.; Malacria, M.; Petit, M., Science of Synthesis Knowledge Updates, (2012) 3, 17. 摘要:Yoshida, H., Science of Synthesis Knowledge Updates, (2022) 3, 3. 摘要:Ferris, G. E.; Mlynarski, S. N.; Morken, J. P., Science of Synthesis Knowledge Updates, (2012) 3, 231.