邻氯苯乙腈置于氢氧化钾,水,铁粉,Potassium Carbonate,溶剂黄146体系中,用 甲醇,乙醇,水,苯 用作溶剂,化学反应 4.0H,反应生成2-氨基-2',5-二氯二苯酮 参考文献:Psychotropic Derivatives Of 5-Phenyl-7-Chloro-1,3-Dihydro-1,4-Benzodiazepin-2-One And Contribution To The Synthesis Of Its 5-(2-Chlorophenyl) Analogue 标题:Psychotropic Derivatives Of 5-Phenyl-7-Chloro-1,3-Dihydro-1,4-Benzodiazepin-2-One And Contribution To The Synthesis Of Its 5-(2-Chlorophenyl) Analogue 摘要:将7-氯-5-苯基-1,3-二氢-1,4-苯二氮杂环己-2-酮(i)与2,5-二甲氧基苯乙酰溴和3-(4-苯基哌嗪基)丙基氯烷基化,得到了诺多西泮(III)和(iv)的n-取代衍生物;化合物(iv)表现出潜在催眠药物的特性.4-氯硝基苯与(2-氯苯基)乙腈在碱性氢氧化物甲醇溶液中反应,得到混合物,从中分离出以下化合物:5-氯-3-(2-氯苯基)-2,1-苯并异噁唑(vii),O-甲氧基肟(x),5-氯-2,3-双(2-氯苯基)吲哚(xi),2-氯-4'-硝基苯基酮(xvii)和2-氯-9-氰基喹啉-N-氧化物(xx).4-氯硝基苯与(2-氟苯基)乙腈进行类似反应,得到化合物xx作为主要产物;少量得到4-硝基苯甲醚,2-氟-4'-硝基苯基酮(xviii)和2-氯喹啉-9-碳腈(xxiv).化合物vii还原为氨基苯基酮衍生物v,经过邻苯二甲酰亚乙酸酰衍生物vi转化为氯代甲基二氮杂西泮ii. Doi:10.1135/cccc19803593
专利号:WO-2024036115-A1 优先权日:2022-08-08 标题:Continuous flow synthesis of lorazepam 发明人:THOMPSON DAVID; BIYANI SHRUTI; HYUN SEOK-HEE; MCGUIRE MICHAEL 权利人:PURDUE RESEARCH FOUNDATION; CONTINUITY PHARMA LLC 摘要:A method for synthesis of Lorazepam in a continuous flow using continuous flow reactor, in which method comprises five steps including N-acylation, diazepine ring closure, imine N- oxidation, Polonovski-type rearrangement, and ester hydrolysis; a green reagent comprising a peroxide reagent and rhenium oxide catalyst for N-oxidation of delorazepam; and an ammonium source combination for the synthesis of delorazepam.
专利号:US-5596001-A 优先权日:1993-10-25 标题 :4-aryl-3-(heteroarylureido)quinoline derivatves 发明人:HAMANAKA ERNEST S 权利人:PFIZER 摘要:Compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein R 1 , R 2 , R 3 , R 4 , m, X and Q are as defined below, and novel intermediates used in the synthesis of such compounds. The compounds of formula I are inhibitors of acyl coenzyme A: cholesterol acyltransferase (ACAT) and are useful as hypolipidemic and natiatherosclerosis agents.
专利号:BE-800340-A 优先权日:1972-06-01 标题:INTERMEDIARIES AND METHODS FOR THE SYNTHESIS OF BENZODIAZEPINES,
专利号:CN-117229206-A 优先权日:2023-09-18 标 题 :A preparation method for base-catalyzed synthesis of multi-substituted 2-quinolinone compounds
专利号:US-4000151-A 优先权日:1974-09-11 标题:Triazolyl benzophenone compounds 发明人:HESTER JR JACKSON B 权利人:UPJOHN CO 摘要:Intermediates of the formula IV: ##STR1## wherein R is selected from the group consisting of hydrogen and alkyl of 1 to 3 carbon atoms, inclusive; and wherein R 2 , R 3 , and R 4 are selected from the group consisting of hydrogen, fluoro, chloro, bromo, nitro, and trifluoromethyl are produced by a multistep synthesis. The final compounds are tranquilizers and sedatives and can be used in mammals, including man, and in birds.
专利号:CN-110606839-B 优先权日:2019-09-30 标题 :Green synthesis method of polysubstituted quinazoline derivative
[参考文献]: F Guan, Et Al. Solid-Phase Microextraction And Gc-Ecd Of Benzophenones For Detection Of Benzodiazepines In Urine. J Anal Toxicol. 1999 Jan-Feb;23(1):54-61.
合成参考文献
摘要:Sharma, U.; Kumar, R.; Gupta, S. S.; Chandra, D., Science of Synthesis Knowledge Updates, (2022) 2, 156. 摘要:Sharma, U.; Kumar, R.; Gupta, S. S.; Chandra, D., Science of Synthesis Knowledge Updates, (2022) 2, 148. 摘要:Sharma, U.; Kumar, R.; Gupta, S. S.; Chandra, D., Science of Synthesis Knowledge Updates, (2022) 2, 237. 摘要:Sharma, U.; Kumar, R.; Gupta, S. S.; Chandra, D., Science of Synthesis Knowledge Updates, (2022) 2, 154. 摘要:Riva, R.; Banfi, L.; Basso, A., Science of Synthesis: Multicomponent Reactions, (2013) 1, 350.