发明名称 ENANTIOSELECTIVE SYNTHESIS OF 6-AMINO-7-HYDROXY-4,5,6,7-TETRAHYDROIMIDAZO[4,5,1-jk][1]BENZAZEPIN-2[1H]-ONE AND ZILPATEROL
摘要 FIELD: chemistry. ^ SUBSTANCE: present invention relates to a method for selective synthesis of 6R,7R trans-stereoisomer of 6-amino-7-hydroxy-4,5,6,7-tetrahydroimidazo[4,5,1-jk][1]benzazepin-2[1H]-one and 6R,7R trans-stereoisomer of zilpaterol or salts thereof for preparing medicinal agents. The disclosed method of producing 6R,7R trans-stereoisomer of 6-amino-7-hydroxy-4,5,6,7-tetrahydroimidazo[4,5,1-jk][1]benzazepin-2[1H]-one involves reaction of 4,5-dihydroimidazo[4,5,1-jk][1]benzazepin-2,6,7[1H]-trione-6-oxime or salt thereof with H2 in the presence of a catalyst which contains a complex of at least one phosphine ligand with at least one metal selected from a group comprising rhodium, ruthenium and iridium. The disclosed method for selective synthesis of the 6R,7R trans-stereoisomer of zilpaterol involves reaction of 4,5-dihydroimidazo[4,5,1-jk][1]benzazepin-2,6,7[1H]-trione-6-oxime with H2 in the presence of a catalyst to form 6-amino-7-hydroxy-4,5,6,7-tetrahydroimidazo[4,5,1-jk][1]benzazepin-2[1H]-one and conversion of the latter to zilpaterol. ^ EFFECT: novel method of producing biologically active compounds. ^ 24 cl, 7 ex, 2 tbl
申请公布号 RU2433131(C2) 申请公布日期 2011.11.10
申请号 RU20090132658 申请日期 2008.01.31
申请人 INTERVET INTERNEHSHNL B.V. 发明人 AL'MENA-PEREHA KHUAN KHOSE;BRINK MONIKA;GAJSS GERKHARD;KADYROV RENAT;MEJER TORSTEN
分类号 A61K31/55;A61P43/00;C07D487/06 主分类号 A61K31/55
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