4-溴苯酚置于溴体系中,用 乙醇,溶剂黄146 用作溶剂,化学反应 1.0H,以87%的收率获得四溴环己二烯-1-酮 参考文献:Triphenylphosphine-2,4,4,6-Tetrabromo-2,5-Cyclohexadienone Complex As A Reagent For Preparation Of Carboxylic Acid Bromides 标题:Triphenylphosphine-2,4,4,6-Tetrabromo-2,5-Cyclohexadienone Complex As A Reagent For Preparation Of Carboxylic Acid Bromides 摘要:成功使用了三苯基膦-2,4,4,6-四溴-2,5-环己二烯酮配合物作为合成羧酸溴化物的新试剂,这些化合物作为单个物质被分离出来或通过转化为相应的酰苯胺来鉴定.该反应具有化学选择性,并且可以应用于多官能团化合物,例如羟基酸. Doi:10.1007/s11178-005-0042-0
专利号:US-8642766-B2 优先权日:2008-05-05 标题 :Synthesis of (+) cortistatin A and related compounds 发明人:SHENVI RYAN A; GUERRERO CARLOS A; SHI JUN; LI CHUANG-CHUANG; BARAN PHIL S 权利人:SHENVI RYAN A; GUERRERO CARLOS A; SHI JUN; LI CHUANG-CHUANG; BARAN PHIL S 摘要:An in vitro synthesis of (+) cortistatin A from readily available precursors is disclosed, as are the syntheses of related 17-aryl substituted compounds, the 17-aryl substituted compounds themselves and novel compounds useful in their preparation.
专利号:US-11512062-B2 优先权日:2018-10-15 标 题:Process for the synthesis of piperazinyl-ethoxy-bromophenyl derivates and their application in the production of compounds containing them 发明人:BEAUREGARD LOUIS-PHILIPPE; BERTRAND MARTIAL; GIGUERE PASCALL; HARDOUIN CHRISTOPHE; SCHIAVI BRUNO 权利人:SERVIER LAB 摘要:Process for the industrial synthesis of the compound of formula (I):
专利号:US-2025101006-A1 优先权日:2022-01-31 标题:Process for the synthesis of pyrazolyl derivatives useful as anti-cancer agents 发明人:BAENZIGER MARKUS; GALLOU FABRICE; GUO FENGFENG; HÄNGGI RUDOLF; HAN ENJIAN; JORDINE GUIDO; LI JIALIANG; LIU WEIPENG; MIAO BUKEYAN; RONG SHAOFENG; SANTANDREA ERNESTO; SCHIRNER PAUL BERND; SHEN XIAODONG; WANG CAN; ZHANG HAO 权利人:NOVARTIS AG 摘要:The invention provides a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially KRAS G12C inhibitors. The present invention provides a direct enantioselective chemical manufacturing method of making Compound A, or a pharmaceutically acceptable hydrate or solvent thereof: (I). The invention provides a process for preparing Intermediate B6* comprising reacting Intermediate B4* with Intermediate B5* in an atroposelective coupling reaction, using a chiral catalyst.
专利号:US-2024010638-A1 优先权日:2020-11-13 标题:Improved synthesis of crac channel inhibitors 发明人:STAUDERMAN KENNETH; DUNN MICHAEL; OLMSTEAD KAY 权利人:CALCIMEDICA INC 摘要:Provided herein is an improved synthetic method for the production of CRAC channel inhibitors. The synthetic method provides a method for producing highly pure CRAC channel inhibitors for clinical testing.
专利号:US-5821387-A 优先权日:1997-12-22 标题 :Polyarenes from aryl ketones with application to synthesis of crisnatol mesylate 发明人:ARCHIBALD THOMAS G; BARNARD JAMES C; HUANG DER-SHING 权利人:AEROJET GENERAL CO 摘要:Alkyl-substituted polyarenes of the formula ##STR1## in which R is alkyl and Ar res is an aryl residue, are prepared from aryl ketones by reaction of the latter with 1-cyclohexenyloxytrimethylsilane in the presence of a Friedel-Crafts catalyst. When R is methyl and Ar res is a naphthyl residue, the reaction serves as a step in a reaction scheme leading to crisnatol mesylate, a pharmaceutical useful in the treatment of brain cancer.
专利号:US-8921580-B2 优先权日:2012-05-09 标 题 :Methods and systems for the formation of cyclic carbonates 发明人:HATTON TREVOR ALAN; JAMISON TIMOTHY F; KOZAK JENNIFER AIDEN; SIMEON FRITZ; WU JIE 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:Described herein are inventive methods for synthesis of cyclic carbonates from CO 2 and epoxide. In some embodiments, the methods are carried out in the presence of a catalyst comprising an electrophilic halogen. In some embodiments, the methods are carried out in a flow reactor.
[参考文献]: Nasser Iranpoor, Et Al. A New Approach To The Reduction Of Sulfoxides To Sulfides With 1,3-Dithiane In The Presence Of Electrophilic Bromine As Catalyst. J Org Chem. 2002 May 3;67(9):2826-30.
合成参考文献
摘要:Wong, Y.-S., Science of Synthesis, (2009) 46, 612. 摘要:Hashmi, A. S. K., Science of Synthesis Knowledge Updates, (2018) 1, 353. 参考文献:10.1021/jo016027y 摘要:Iranpoor N, Firouzabadi H, Shaterian HR. A new approach to the reduction of sulfoxides to sulfides with 1,3-dithiane in the presence of electrophilic bromine as catalyst. J Org Chem. 2002 May 03;67(9):2826–30. doi: 10.1021/jo016027y. 摘要:Hilp M. 1,3-Dibromo-5,5-dimethylhydantoin (DBH) as oxidant and precipitant for drug identification according to PH. EUR Analytical methods of pharmacopoeias with DBH in respect of environmental and economical concern, Part 15(1). Pharmazie. 2002 Jun;57(6):393–5.