| 摘要 |
The invention comprises amines of the general formula <FORM:1094235/C2/1> wherein R1 and R2, identical or different, each stand for a hydrogen atom, lower alkyl (C1-C4), cycloalkyl or dialkylaminoalkyl or R1 and R2 are linked together to one carbon chain which may be interrupted by a hetero atom and substituted, thus forming together with the nitrogen atom a heterocyclic saturated residue and salts thereof and a process for the preparation thereof wherein 10 - chloro - 10,11 - dihydro-dibenzo (b, f) thiepin is brought into reaction with a substance of the formula R1R2NH, wherein R1 and R2 are as defined above and the product optionally converted to a salt with a pharmaceutically convenient acid. Examples describe the preparations of 10-dimethylamino-, 10-amino-, 10-methylamino-, 10-diethylamino-10-piperidino-, 10-(4-phenyl-4-carbethoxypiperidino-, 10-(4-methylpiperazino-, 10-(methyl-hexahydro - 1,4 - diazepin) -, 10 - piperazino - and 10 - (4 - ethylpiperazino) - 10,11 - dihydrodibenzo (b,f) thiepins some of which are isolated as hydrochlorides or maleates. 10 - Chloro - 10,11 - dihydrodibenzo (b,f) thiepin employed as starting material is obtained by reacting diphenylsulphide - o - carboxylic acid with lithium-aliminium hydride, decomposing the product to obtain o - hydroxymethyl-diphenylsulphide, converting the latter successively to the corresponding o-chloro-, o-cyano- and -o-acetic acid compounds, treating the latter with polyphosphoric acid to obtain 10,11 - dihydrodibenzo (b, f) thiepin - 10 - on, reducing the latter with sodium borohydride to the corresponding hydroxy compound and converting the latter to the corresponding 10-chloro-compound by reaction with thionyl chloride. |
