abstract |
NEW MATERIAL:The 2-nitroimidazole derivative of formula I [R 1 is -(CH 2 ) n -OR 2 , -CH 2 CH=CHCH 2 -OR 2 or -CH 2 C=CCH 2 -OR 2 (n is 3 or 4; R 2 is H or acyl)]. n EXAMPLE: 1-[(4'-Acetoxybutoxy)methyl]-2-nitroimidazole. n USE: An antifilarial agent, antitrichomonas agent, antibacterial agent and radiation sensitizer. n PROCESS: The 2-nitroimidazole of formula II (X is H, alkali metal or trialkylsilyl) is made to react with compound of formula III [Y is halogen; R 3 is -(CH 2 ) n -OR 4 , -CH 2 CH=CHCH 2 -OR 4 or -CH 2 C=CCH 2 -OR 4 (R 4 is acyl)] to obtain the compound of formula I a, which is deacylated to the compound of formula I b [R 5 is -(CH 2 ) n -OH, -CH 2 CH=CHCH 2 -OH or -CH 2 C=CCH 2 -OH]. n COPYRIGHT: (C)1984,JPO&Japio |