abstract |
NEW MATERIAL:A compound shown by formula I {X is O, methylene, S or -NR 5 -; R 1 and R 2 are H, halogen, lower alkyl, lower alkoxy, etc.; one of R 3 and R 4 is group shown by formula II [-Y- is -(CH 2 ) n - (n is 0 or 1) or -NR 6 -] and the other is H, lower alkyl, (substituted) aromatic or heterocyclic ring; R 5 and R 6 are H, lower alkyl, acyl, etc.; broken line is single bond or double bond}. n EXAMPLE: 5-(4,5-Dihydro-1H-imidazol-2-y1)-2,3,4,5-tetrahydrobenzoxepin hydrochloride. n USE: A medicine for diabetes having excellent blood sugar lowering action and inhibitory action on blood platelet aggregation. n PREPARATION: A compound shown by formula III is subjected to cyanophosphonation, then reacted with boron trifluoride ether complex to give an α,β-unsaturated nitrile derivative shown by formula IV, which is reacted with p-toluenesulfonate of ethylenediamine under heating. n COPYRIGHT: (C)1992,JPO&Japio |