专利号:US-8557981-B2 优先权日:2010-05-04 标题:Process for the synthesis of 4H-imidazo [1,5-a] [1,4] benzodiazepines, in particular midazolam and salts thereof 发明人:CASTELLIN ANDREA; MAGGINI MICHELE; DONNOLA PAOLA 权利人:CASTELLIN ANDREA; MAGGINI MICHELE; DONNOLA PAOLA; ITALIANA SINT SPA 摘要:The present invention refers to a process for the preparation of 4H-imidazo[1,5-a][1,4]benzodiazepines, in particular Midazolam, through an efficient and selective decarboxylation reaction of the derivative compound of the 5-aminomethyl-1-phenyl-1H-imidazole-4-carboxylic acid of formula (II) n navoiding the formation of the 6H-imidazo[1,5-a][1,4]benzodiazepines by-products and the ensuing process for the isomerization of a 4H-imidazo[1,5-a][1,4]benzodiazepine product.
专利号:US-2011275799-A1 优先权日:2010-05-04 标题:PROCESS FOR THE SYNTHESIS OF 4H-IMIDAZO [1,5-a] [1,4] BENZODIAZEPINES, IN PARTICULAR MIDAZOLAM AND SALTS THEREOF
专利号:EP-2397470-B1 优先权日:2010-05-04 标题:Process for the synthesis of 4H-imidazo[1,5-a][1,4]benzodiazepines, in particular midazolam and salts thereof
专利号:IT-MI20100777-A1 优先权日:2010-05-04 标 题 :PROCEDURE FOR THE SYNTHESIS OF 4H-IMIDAZO [1,5-A] [1,4] BENZODIAZEPINE, IN PARTICULAR OF MIDAZOLAM.
专利号:IL-212505-A 优先权日:2010-05-04 标题:Process for Synthesis of 4h - Imidazo [5,1– a] [4,1] Benzodiazepines, especially Midazolam and its salts
专利号:EP-2397470-A1 优先权日:2010-05-04 标题 :Process for the synthesis of 4H-imidazo[1,5-a][1,4]benzodiazepines, in particular midazolam and salts thereof
1: Ganter M, Kanngiesser M. Auswirkung von Ketamin und dessen Kombinationen mit Xylazin und Climazolam auf Kreislauf und Atmung beim Schwein [Effect of ketamine and its combinations with xylazine and climazolam on the circulation and respiration in swine]. Zentralbl Veterinarmed A. 1991 Aug;38(7):501-9. German. 21(2):143-8. doi: 10.1177/002367728702100211. 149(9):395-402. doi: 10.1024/0036-7281.149.9.395. 57(10):1472-7. 67(1):152-9. doi: 10.2460/ajvr.67.1.152. 36(4):417-9. 132(5):251-7. German. 10(2):65-8. doi: 10.1002/(SICI)1099-0801(199603)10:2<65::AID- BMC555>3.0.CO;2-Q. 162(2):308-13. doi: 10.1016/j.jss.2009.03.007. Epub 2009 Apr 10. 12(2):147-56. doi: 10.1111/j.1365-2885.1989.tb00656.x.
合成参考文献
参考文献:10.1177/002367728702100211 摘要:West CD, Green CJ. The sedative effects of climazolam and climazolam with fentanyl-fluanisone in rats (Rattus norvegicus). Lab Anim. 1987 Apr;21(2):143–8. doi: 10.1177/002367728702100211. 参考文献:10.2460/ajvr.1996.57.10.1472 摘要:Bettschart-Wolfensberger R, Taylor PM, Sear JW, Bloomfield MR, Rentsch K, Dawling S. Physiologic effects of anesthesia induced and maintained by intravenous administration of a climazolam-ketamine combination in ponies premedicated with acepromazine and xylazine. ajvr. 1996 Oct 01;57(10):1472–7. doi: 10.2460/ajvr.1996.57.10.1472.