| 摘要 |
1,144,970. Tricyclic aminomethyl derivatives. BOEHRINGER MANNHEIM G.m.b.H. 20 Dec., 1967 [23 Dec., 1966], No. 57916/67. Heading C2C. Novel compounds of Formula I, in which X is a sulphur atom or an oxymethylene, thiomethylene, thioethylene or trimethylene radical, R 1 is a hydrogen or halogen atom or a C 1-3 alkyl, alkoxy, trifluoromethyl or alkylthio radical and each of R 2 , R 3 and R 4 is a hydrogen atom or a C 1-3 alkyl radical, and salts thereof with physiologically compatible acids, are prepared by (a) subjecting a carboxylic acid of Formula II, or an appropriate reactive derivative thereof, to the Hofmann, Curtius, Lossen or Schmidt rearrangement, and, if necessary, hydrolysing a resulting isocyanate, or (b) reducing a Schiff's base, aldehyde-ammonia compound, hydrazone or oxime of a carbonyl compound of Formula III, or (c) reducing a nitrile of Formula IV, or a corresponding carbonamide (to give a compound in which R 2 is hydrogen) or (d) alkylating a compound of Formula I, produced according to reaction (a), (b) or (c), in which R 3 and/or R 4 are hydrogen atoms. Thiaxanthene-9-carboxamide is prepared by reacting thiaxanthene-9-carboxylic acid with thionyl chloride followed by ammonia. 11 - Cyano - 6,11 - dihydro - dibenz - [b,e]- oxepin is prepared by reacting 11-hydroxy-6,11- dihydro-dibenz-[b,e]-oxepin with thionyl chloride followed by sodium cyanide. 11 - Acetyl - 6,11 - dihydro - dibenz - [b,e]- oxepin is prepared by reacting 6,11-dihydrodibenz-[b,e]-oxepin-11-one with ethyl magnesium bromide to form 11-hydroxy-11-ethyl-6,11-dihydro-dibenz-[b,e]-oxepin, treating this with alcoholic hydrochloric acid to give 11-ethylene- 6,11-dihydro-dibenz-[b,e]-oxepin, heating this with formic acid and hydrogen peroxide to give 11 - hydroxy - 11 - (1 - hydroxyethyl) - 6,11 - dihydro-dibenz-[b,e]-oxepin, and heating this with sulphuric acid.
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