Alkaline Earth Salt Of/the/ Methylsulfuric Acid置于五氯化磷体系中,化学反应生成2-溴苯磺酰氯 参考文献:Berndsen; Limpricht,Justus Liebigs Annalen Der Chemie,1875,Vol. 177,P. 101 标题:Berndsen; Limpricht,Justus Liebigs Annalen Der Chemie,1875,Vol. 177,P. 101
专利信息
专利号:US-2025188046-A1 优先权日:2023-12-08 标题:Ultrafast flow synthesis of functionalized sulfonyl fluorides and subsequent sufex connections via lithiated chemistry 发明人:KIM DONG-PYO; KANG JI-HO 权利人:POSTECH RES & BUSINESS DEV FOUND 摘要:Disclosed are ultrafast flow synthesis of functionalized sulfonyl fluorides and subsequent SuFEx connections via lithiated chemistry. In detail, a method of synthesizing an ortho-functionalized benzenesulfonyl fluoride derivative, the method comprises (a) reacting a benzenesulfonyl fluoride derivative represented by structural formula 1 with an organolithium represented by structural formula 2, thus synthesizing an intermediate represented by structural formula 3 in reaction scheme 1 and (b) reacting the intermediate with an electrophile, thus synthesizing a compound represented by structural formula 4 or a compound represented by structural formula 4′. The present disclosure enables the synthesis of several functionalized sulfonyl fluorides within a few seconds under mild temperature conditions in addition to the chemistry of Sulfonyl Fluoride Exchange (SuFEx), which is a next-generation click chemistry, so that sulfonyl fluoride, the main reactant of the SuFEx reaction, can be efficiently secured.
专利号:US-6388083-B2 优先权日:2000-07-07 标题 :Process for the synthesis of (2S)-phenyl-3-piperidone 发明人:LEE JAEMOON; ASKIN DAVID; HOANG THOA 权利人:MERCK & CO INC 摘要:The present invention is concerned with novel processes for the preparation of (2S)-phenyl-3-piperidone. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.
专利号:US-7439364-B2 优先权日:2001-05-17 标 题 :Process for the synthesis of derivatives of halo-[2,3-F] quinoline 发明人:CHAN ANITA W; CURRAN TIMOTHY T; IERA SILVIO; CHEW WARREN; SELLSTEDT JOHN H; VID GALINA; FEIGELSON GREG; DING ZHIXIAN 权利人:WYETH CORP 摘要:Methods of preparing compounds of Formula I n nare provided.
专利号:WO-2014170910-A1 优先权日:2013-04-04 标 题:Process for the preparation of lapatinib 发明人:MUDDASANI PULLA REDDY; TALASILA SAMBASIVA RAO; SATTI VENKATA REDDY; NEKKANTI SATISH CHOWDARY; NANNAPANENI VENKAIAH CHOWDARY 权利人:NATCO PHARMA LTD 摘要:Present process relates to an improved and commercial process for the preparation of lapatinib of formula-I or its pharmaceutically acceptable p-toluenesulfonate salt involving novel intermediates of formulae-XVII, XVIII, and XIX. Present process utilizes Meerwein reaction as a key step in the aryl C-C bond formation step avoiding costly boronate coupling chemistry used in the conventional synthesis of lapatinib.
专利号:US-6943254-B2 优先权日:1997-03-07 标 题 :Synthesis of pyrazinyl pyridine-3-sulfonamide compounds 发明人:HOGAN PHILIP JOHN 权利人:ASTRAZENECA UK LTD 摘要:A process for the manufacture of: n n nwherein R is (1-4C)alkyl, carboxyl(1-4C)alkyl or 1,3,4-oxadiazol-2-yl comprises:n (a) reaction of the diazonium salt of 3-amino-2-chloropyridine with thionyl chloride in water and an electron transfer catalyst; (b) reaction with isobutyl-(3-methoxy-5-methylpyrazin-2-yl)carbamate and an alkali metal hydride in inert solvent; and (I) where R is (1-4C)alkyl, carboxy(1-4C)alkyl: (c) reaction with a boronic acid: n n (or an anhydride or ester therof) in the presence of a base and a palladium or nickel catalyst in solvent; and removal of the isobutoxy carbonyl group; or (ii) where R is 1,3,4-oxadiazol-2-yl (c) reaction with 4-methoxycarbonylphenylboronic acid (or an anhydride or ester thereof) with a source fluoride ion under aqueous conditions; (d) removal of the isobutoxycarbonyl protecting group; (e) conversion of the methyl ester group to the hydrazide; and (f) conversion to a 1,3,4-oxadiazol-2-yl moiety.
专利号:US-2002187983-A1 优先权日:2001-05-17 标 题:Process for the synthesis of derivatives of 2, 3-dihydro-1, 4-dioxino- [2, 3-f] quinoline
摘要:Kawęcki, R., Science of Synthesis Knowledge Updates, (2018) 4, 296. 摘要:Andersson, C.-M.; Andersson, M., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 3, 8. 摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2025).