| 摘要 |
<p>1,126,354. Tetrahydroisoquinoline derivatives. SANDOZ Ltd. 13 Aug., 1965 [24 Aug., 1964], No. 3328/68. Divided out of 1,126,352. Heading C2C. Racemic and optically active compounds of the general Formula (XII) (wherein each of R 1 and R 2 represents a hydrogen atom or a methoxy group, each of R 3 and R 4 represents a hydrogen atom or a methyl group, R<SP>1</SP> 6 represents a hydrogen atom or a C 1-4 alkyl group and X represents a chlorine atom or a trifluoromethyl group or-when R<SP>1</SP> 6 is an alkyl group-a hydrogen atom) and their acid addition salts are prepared by (a) reducing a racemic or optically active compound of the Formula (XI) or (b)-when R<SP>1</SP> 6 represents a hydrogen atom-reducing a racemic or optically active compound of the Formula (VII) optionally followed in either case by salt formation and/or resolution. Compounds (XI) may be prepared by (a) subjecting a compound of the Formula (X) to Bischler-Napieralski ring closure, the amino group being protected prior to ring closure and the protecting group removed after ring closure, or (b) reacting a compound of the Formula (XV) (wherein Hal represents a chlorine or bromine atom) with R<SP>1</SP> 6 NH 2 at 50-60‹ C. in the presence of copper powder and cuprous chloride. Compounds (X) may be prepared by condensing a compound of the Formula (IV) with a compound of the Formula (IXa) (wherein R represents a C 1-4 alkyl group) or (IXb) Compounds (VII) may be prepared by subjecting a compound of the Formula (VI) to Bischler-Napieralski ring closure. Compounds (VI) may be prepared by condensing a compound of the Formula (IV) with a compound of the Formula (V) in an alkaline medium. Compounds (XV) may be prepared by heating a compound of the Formula (XIII) with a compound of the Formula (XIV)</p> |
