申请人:PFIZER INC.
公开号:EP0082658A2
公开(公告)日:1983-06-29
1,1-Di(p-fluorophenyl)urea, 2-carbobenzoxy-8-fluoro-5-(p-fluorophenyl)-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole, an efficient process for converting the former to the latter, further comprising conversion of the latter to 8-fluoro-5-(p-fluorophenyl)-2-[4-(p-fluorophenyl)-4-hydroxybutyl)]-2,3,4,5-tetrahydro-1 H-pyrido[4,3-b]indole (flutroline) or to 8-fluoro-5-(p-fluorophenyl]-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole (an alternative flutroline intermediate); and further, novel processes and intermediates used in converting the latter to flutroline.
1,1-二(对氟苯基)脲,2-苄氧基-8-氟-5-(对氟苯基)-2,3,4,5-四氢-1H-吡啶并[4,3-b]吲哚,将前者转化为后者的高效工艺、进一步包括将后者转化为 8-氟-5-(对氟苯基)-2-[4-(对氟苯基)-4-羟基丁基)]-2,3,4,5-四氢-1H-吡啶并[4,3-b]吲哚(氟脯氨酸)或 8-氟-5-(对氟苯基)-2,3,4,5-四氢-1H-吡啶并[4,3-b]吲哚(另一种氟脯氨酸中间体);以及用于将后者转化为氟脯氨酸的新型工艺和中间体。