| 摘要 |
Compounds of formula I <IMAGE> wherein Y is -CH2F, -CHF2, -CH2Cl or -CHCl2; R is hydroxy, alkoxy, amino alkylamino, dialkylamino or carboxyalkylamino, R1 is hydrogen, alkylcarbonyl, alkoxycarbonyl or aminoalkylcarbonyl, and three of R2, R3, R4, R5 and R6 are hydrogen and the other two are selected from hydroxy, methyl and methoxy, and salts thereof. Also disclosed is a process of preparing compounds of formula I in which R is hydroxy, R1 is hydrogen, Y is -CH2F and R2, R3, R4, R5 and R6 are various combinations of hydrogen, methyl, ethyl, halogen, trifluoromethyl, hydroxy, methoxy and methylenedioxy by reacting a novel ketone of formula III <IMAGE> wherein R12 to R16 correspond to R2 to R6 provided that hydroxy groups are protected, with sodium cyanide and an ammonium salt, and hydrolysing the resulting aminonitrile. The novel ketones are prepared by reacting a suitable benzyl Grignard with fluoroacetonitrile and hydrolysing the resulting ketimine. |
