发明名称 Process for preparation of (S)-N,N'-bis[2-hydroxy-1- (hydroxymethyl)ethyl]-5-[(2-hydroxy-1-oxopropyl)amino]-2,4,6- triiodo-1,3-benzendicarboxamide and intermediates
摘要 <p>A process for the preparation of (S)-N,N'-bis[2-hydroxy-1- (hydroxymethyl)ethyl]-5-[(2-hydroxy-1-oxopropyl)amino]-2,4,6- triiodo-1,3-benzendicarboxamide of formula (l) starting from a compound of formula (II) which process comprises a) reacting the compound of formula (II) with a suitable protecting agent, to give a compound of formula (III), wherein R is a group of formula A or B, wherein R1 is a hydrogen atom, a C1-C4 straight or branched alkyl group or a C1-C4 straight or branched alkoxy group, R2 is hydrogen, a C1-C4 straight or branched alkyl group or a C1-C4 straight or branched alkoxy group and R3 is a C1-C4 straight or branched alkyl group, a trifuoromethyl or a trichloromethyl group; b) acylating the amino group in position 5 of the intermediate compound of formula (III), by reaction with a (S)-2-(acetyloxy)propanoyl chloride to give a compound of formula (IV), wherein R is as defined above; and c) removing all the acyl groups present in the compound of formula (IV) under basic conditions, without isolating the compound of formula (IV).</p>
申请公布号 SK287570(B6) 申请公布日期 2011.03.04
申请号 SK20030000656 申请日期 2001.11.29
申请人 BRACCO IMAGING S.P.A. 发明人 ANELLI PIER LUCIO;BROCCHETTA MARINO;LUX GIOVANNA;CAPPELLETTI ENRICO
分类号 C07C237/46;A61K49/04;C07B51/00;C07C231/02;C07C231/12;C07D319/06 主分类号 C07C237/46
代理机构 代理人
主权项
地址