专利号:US-8629134-B2 优先权日:2007-02-01 标题:Enantioselective synthesis of 6-amino-7-hydroxy-4,5,6,7-tetrahydro-imidazo[4,5,1-jk][1]-benzazepin-2[1H]-one and zilpaterol 发明人:ALMENA-PEREA JUAN JOSE; BRINK MONIKA; GEIBETA GERHARD; KADYROV RENAT; MEYER THORSTEN 权利人:ALMENA-PEREA JUAN JOSE; BRINK MONIKA; GEIBETA GERHARD; KADYROV RENAT; MEYER THORSTEN; INTERVET INT BV 摘要:This invention relates to a process for the hydrogenation of a ketooxime to selectively form an aminoalcohol stereoisomer, and, in particular, to a process for the hydrogenation of 4,5-dihydro-imidazo[4,5,1-jk][1]benzazepin-2,6,7[1H]-trione-6-oxime or a salt thereof to selectively form a stereoisomer of 6-amino-7-hydroxy-4,5,6,7-tetrahydro-imidazo[4,5,1-jk][1]-benzazepin-2[1H]-one or a salt thereof. This invention also relates to the use of the 6-amino-7-hydroxy-4,5,6,7-tetrahydro-imidazo[4,5,1-jk][1]-benzazepin-2[1H]-one hydrogenation product or a salt thereof to selectively make a stereoisomer of zilpaterol or a salt thereof, as well as the use of such a zilpaterol stereoisomer or salt in methods of treatment and medicaments for animals.
专利号:US-11214551-B2 优先权日:2018-04-27 标题 :One pot synthesis of 4-(1,2-dihydro-2-oxobenzo[d]imidazol-3-yl)butanoic acid, a key intermediate of zilpaterol 发明人:RAVI KUMAR KANNASANI; MALLIK YADAV KASA; SREENU MULU; BABU V V V 权利人:RA CHEM PHARMA LTD 摘要:The present invention relates to one pot process for the preparation of 4-(1,2-dihydro-2-oxobenzo[d]imidazol-3-yl)butanoic acid of Formula-I, which is a key intermediate and its use in the preparation of Zilpaterol, which comprises condensation of methyl-4-chloro butyrate with 1-(prop-1-en-2-yl)-1H-benzo[d]imidazol-2(3H)-one in presence of a base and suitable solvent to give corresponding ester derivative, further hydrolyzation and acidification in presence of inorganic solvent to obtain Formula-I.
专利号:BR-112020021893-A2 优先权日:2018-04-27 标题:synthesis of a single container of 4- (1,2-dihydro-2-oxobenzo [d] imidazol-3-yl) butanoic acid, a key intermediate of zilpaterol
专利号:MX-2020011336-A 优先权日:2018-04-27 标题:SINGLE VESSEL SYNTHESIS OF 4-(1,2-DIHYDRO-2-OXOBENZO [D]IMIDAZOL-3-IL)BUTANOIC ACID, A KEY INTERMEDIATE OF ZILPATEROL.
专利号:WO-2019207591-A1 优先权日:2018-04-27 标 题 :One pot synthesis of 4-(1,2-dihydro-2-oxobenzo[d]imidazol-3-yl)butanoic acid, a key intermediate of zilpaterol
专利号:AU-2008209743-A1 优先权日:2007-02-01 标 题:Enantioselective synthesis of 6-amino-7-hydroxy-4, 5, 6, 7-tetrahydro-imidazo [4, 5, 1-jk] [1] -benzazepin-2 [1H] -one and zilpaterol
参考文献:10.1007/s11743-011-1262-7 摘要:Lakhrissi L, Hassan N, Lakhrissi B, Massoui M, Essassi EM, Ruso JM, Solans C, Rodriguez‐ Abreu C. Surfactants Based on Bis‐Galactobenzimidazolones: Synthesis, Self‐Assembly and Ion Sensing Properties. J Surfact & Detergents. 2011 Mar 15;14(4):487–95. doi: 10.1007/s11743-011-1262-7. 参考文献:10.1055/s-0037-1611439 摘要:Synthesis of Flibanserin. Synfacts. 2018 Dec 14;15(01):0008. doi: 10.1055/s-0037-1611439.