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-6998484-B2 优先权日:2000-10-04 标 题:Synthesis of purine locked nucleic acid analogues 发明人:KOCH TROELS; JENSEN FLEMMING REISSIG 权利人:SANTARIS PHARMA AS 摘要:The present invention relates to a new method for the synthesis of purine LNA (Locked Nucleic Acid) analogues which provides a higher overall yield. The method comprising a regioselective 9-N purine glycosylation reaction followed by a one-pot nucleophilic aromatic substitution reaction of the 6-substituent in the purine ring and simultaneous nucleophile-induced intramolecular ring closure of the C-branched carbohydrate to form novel purine LNA analogues. The novel strategy is illustrated by the synthesis of the novel compound (1S,3R,4R,7S)-7-benzyloxy-1-methanesulfonylmethyl-3-(guanin-9-yl)-2,5-dioxabicyclo[2.2.1]heptane which is easily converted into (1S,3R,4R,7S)-7-hydroxy-1-hydroxymethyl-3-((2-N-isobutyrylguanin-9-yl)-2,5-dioxabicyclo[2.2.1]heptane after isobutyryl protection of the 2-amino purine group and subsequent substitution of 1-methanesulfonyl with benzoate, debenzoylation and debenzylation.
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.
专利号:US-12281398-B2 优先权日:2022-02-07 标题:Microfluidic process for the general electrochemical synthesis of geminal dipseudohalide or halide-pseudohalide compounds 发明人:SCHROER THORSTEN G; LECROY GREGORY E; AGUILA MIGUEL; RODRIGUEZ MAYRA P; DOWNARD TYLER J; MACLEOD BRIANNA L 权利人:US GOV AIR FORCE; US AIR FORCE 摘要:A process for the microfluidic electrochemical synthesis of geminal dipseudohalide or halide-pseudohalide compounds comprising the steps ofpumping a solution comprising a compound of Formula Iinto a microfluidic electrochemical reactor in the presence of a base, one of a halide or pseudohalide salt (MY), and a mediator;applying an electrical current through the microfluidic electrochemical reactor; andperforming oxidative addition to create a geminal dipseudohalide or halide-pseudohalide compound of the general Formula II
专利号:US-6348616-B1 优先权日:1996-07-26 标题 :Practical synthesis of benzoxazinones useful as HIV reverse transcriptase inhibitors 发明人:PIERCE MICHAEL ERNEST; RADESCA LILIAN ALICIA 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 the formula:is particularly effective in the treatment of HIV.
专利号:US-5932726-A 优先权日:1996-12-16 标 题 :Asymmetric synthesis of benzoxazinones 发明人:PIERCE MICHAEL ERNEST; CHOUDHURY ANUSUYA; PARSONS JR RODNEY LAWRENCE; RADESCA LILIAN ALICIA 权利人:DU PONT PHARM CO 摘要:The present invention provides novel methods for the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one of formula (VI-i) ##STR1## which is useful as a human immunodeficiency virus (HIV) reverse transcriptase inhibitor.
[参考文献]: Mijung Kim, Et Al. Pharmacologic Alternatives To Riboflavin Photochemical Corneal Cross-Linking: A Comparison Study Of Cell Toxicity Thresholds. Invest Ophthalmol Vis Sci. 2014 Apr 10;55(5):3247-57. [参考文献]: Robin C Anderson, Et Al. Effects Of Select Nitrocompounds On In Vitro Ruminal Fermentation During Conditions Of Limiting Or Excess Added Reductant. Bioresour Technol. 2008 Dec;99(18):8655-61.
合成参考文献
摘要:Yoshimatsu, M., Science of Synthesis Knowledge Updates, (2016) 2, 400. 摘要:Yliniemelä-Sipari, S. M.; Pihko, P. M., Science of Synthesis: Stereoselective Synthesis, (2011) 2, 662. 摘要:Xiao, X., Science of Synthesis: Knowledge Updates, (2023) 2, 132. 参考文献:10.1186/s40104-017-0145-9 摘要:Patra A, Park T, Kim M, Yu Z. Rumen methanogens and mitigation of methane emission by anti-methanogenic compounds and substances. Journal of Animal Science and Biotechnology. 2017 Jan 26;8(1):13. doi: 10.1186/s40104-017-0145-9. 参考文献:10.1016/j.biortech.2008.04.064 摘要:Anderson RC, Krueger NA, Stanton TB, Callaway TR, Edrington TS, Harvey RB, Jung YS, Nisbet DJ. Effects of select nitrocompounds on in vitro ruminal fermentation during conditions of limiting or excess added reductant. Bioresour Technol. 2008 Dec;99(18):8655–61. doi: 10.1016/j.biortech.2008.04.064.