NEW MATERIAL:An acylated indole derivative of formula I (R1 is H or lower alkyl; R2 is 2W6C lower alkyl; R3 is H, OH, halogen, lower alkyl or lower alkoxy; Z is phenyl or R3-substituted phenyl; A is H, lower alkyl or lower acyl; n is an integer of (1W5), its optically active isomer or its salt.
EXAMPLE: 3-Benzoyl-1-(1-hydroxy-2-hexyl)-2-methylindole.
USE: Prevention of cardiovascular infarction, prevention of post-operative thrombosis, remedy and prevention of arteriosclerosis, etc. It suppresses the coagulation of blood platelet, and has low activity to form gastroenteric ulcer.
PROCESS: The compound of formula I is prepared by the condensation reaction of an indole derivative of formula II (R31 is H, halogen, lower alkyl, etc.; A1 is lower alkyl or lower alkoxy) with an acid anhydride of formula III (Z1 is R31-substituted phenyl) in the presence of HI, optionally followed by hydrolysis.
YUU TAKESHI
OOBA TAKEO
TANAKA TOSHIO
WATANABE KENZOU
SAKAUCHI KIYOSHI
KUROZUMI SEIJI
OOTSU AKIRA
NARITOMO TATSUYUKI
SUZUKI YOSHIKI
| JPS5663960A | 1981-05-30 | |||
| JPS56108765A | 1981-08-28 | |||
| JPS54160311A | 1979-12-19 | |||
| JPS5639068A | 1981-04-14 |