专利号:US-10189803-B2 优先权日:2008-02-22 标题 :Synthesis of therapeutic and diagnostic drugs centered on regioselective and stereoselective ring opening of aziridinium ions 发明人:CHONG HYUN-SOON 权利人:CHONG HYUN SOON; ILLINOIS INSTITUTE OF TECH 摘要:Stereoselective and regioselective synthesis of compounds via nucleophilic ring opening reactions of aziridinium ions for use in stereoselective and regioselective synthesis of therapeutic and diagnostic compounds.
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-6177564-B1 优先权日:1998-09-11 标题:Process for the synthesis of N-benzyl-3-(4-fluorophenyl)-1-4-oxazin-2-one 发明人:NELSON TODD D; BHUPATHY MAHADEVAN 权利人:MERCK & CO INC 摘要:The present invention is concerned with a novel process for the preparation of N-benzyl-3-(4-fluorophenyl)-1,4-oxazin-2-one of the formula:This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity, in particular, as substance P (neurokinin-1) receptor antagonists.
专利号:US-12037623-B2 优先权日:2018-07-09 标 题 :Enzymatic synthesis of 4′-ethynyl nucleoside analogs 发明人:HUFFMAN MARK A; FRYSZKOWSKA ANNA; KOLEV JOSHUA N; DEVINE PAUL N; CAMPOS KEVIN R; TRUPPO MATTHEW; NAWRAT CHRISTOPHER C 权利人:MERCK SHARP & DOHME; MERCK SHARP & DOHME LLC 摘要:The present invention relates to an enzymatic synthesis of 4′-ethynyl-2′-deoxy nucleosides and analogs thereof, for example EFdA, that eliminates the use of protecting groups on the intermediates, improves the stereoselectivity of glycosylation and reduces the number of process steps needed to make said compounds. It also relates to the novel intermediates employed in the process.
专利号:US-6600040-B2 优先权日:2000-06-08 标 题:Process for the synthesis of (2R, 2-alpha-R, 3A)-2-[1-(3,5-bis(trifluoromethyl)phenyl)ethoxy]-3-(4-fluorophenyl)-1, 4-oxazine 发明人:BRANDS KAREL M JOS; TSAY FUH-RONG; CONRAD KAREN M; ZHAO MATTHEW M 权利人:MERCK & CO INC 摘要:The present invention is concerned with novel processes for the preparation of (2R, 2-alpha-R, 3a)-2-[1-[3,5-bis(trifluoromethyl)phenyl]ethoxy-3-(4-fluorophenyl)-1,4-oxazine. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.
专利号:US-6395898-B1 优先权日:2000-06-09 标 题:Trans-glycosidation process for the synthesis of (2R, 2-alpha-R, 3a)-2-[1-(3,5-bis(trifluoromethyl)phenyl)ethoxy]-3-(4-fluorophenyl)-1,4-oxazine 发明人:MCNAMARA JAMES M; ZHAO MATTHEW M 权利人:MERCK & CO INC 摘要:The present invention is concerned with novel processes for the preparation of (2R, 2-alpha-R, 3a)-2-[1-[3,5-bis(trifluoromethyl)phenyl]ethoxy-3-(4-fluorophenyl)-1,4-oxazine. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.
[参考文献]: E R Kennedy, Et Al. Determination Of Formaldehyde In Air As An Oxazolidine Derivative By Capillary Gas Chromatography. Anal Chem. 1982 Sep;54(11):1739-42.
合成参考文献
摘要:Dekeukeleire, S.; D'hooghe, M.; De Kimpe, N., Science of Synthesis Knowledge Updates, (2011) 3, 114. 摘要:Vashchenko, B. V.; Grygorenko, O. O., Science of Synthesis Knowledge Updates, (2021) 3, 353. 摘要:Scholz, U.; Dong, W.; Feng, J.; Shi, W., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 45. 摘要:Carboni, B.; Berrée, F., Science of Synthesis: Multicomponent Reactions, (2013) 1, 229.