| 摘要 |
1446093 Aminoalkyl - indole derivatives SCHERICO Ltd 3 Dec 1973 [13 Dec 1972] 55819/73 Heading C2C [Also in Division A5] Novel compounds I (Alk is a 1-4C saturated, divalent, acyclic hydrocarbon group, cyclopropylidene or cyclopropylene; X is halo, NO 2 , OMe or CF 3 ; Y is H or halo, but if X is NO 2 , Y must be halo ; M is H, halo, Me or CF 3 ; and Z is H, halo, NO 2 or Me; provided Y is halo and X is at the 5-position when at least one of M and Z is H) and acid addition salts thereof are prepared by (1) reduction of a compound III (Pg is H or a protecting group and Q is a group directly reducible to -alkNH 2 ) or (2) removal of the amino blocking group or groups from a compound IV (R<SP>4</SP>, R<SP>5</SP> and R<SP>6</SP> are H or a blocking group, at least one being other than H). Intermediates isolated are N-[2-(2,6-difluorobenzoyl) - 4 - chlorophenyl] - glycinonitrile prepared by reaction of 2-amino-5-chloro-2<SP>1</SP>,6<SP>1</SP>- difluorobenzophenone with KCN and paraformaldehyde and 5 - chloro - 3 - (2,6 - difluorophenyl) - indole - 2 - carbonitrile prepared by cyclization of the first named intermediate. |
