Basic derivatives of tricyclic compounds and methods for...

C - Chemistry – Metallurgy – 07 – D

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C07D 327/02 (2006.01) C07C 29/147 (2006.01) C07C 33/46 (2006.01) C07C 45/00 (2006.01) C07C 45/29 (2006.01) C07C 47/575 (2006.01) C07D 211/22 (2006.01) C07D 321/10 (2006.01) C07D 339/00 (2006.01) C07D 411/06 (2006.01)

Patent

CA 1186313

ABSTRACT OF THE DISCLOSURE: The invention comprises compounds and methods of preparation of a large area of basic derivatives of linearly condensed tricyclic systems formed by two external benzene nuclei and a central seven-membered ring with two chalcogen atoms as hetero atoms When both of the chalocogens are atoms of oxygen, we are dealing with derivatives of 11H- dibenzo(b,e)-1,4-dioxepin; when both of the chalcogens are sulfur atoms, we are dealing with derivatives of 11H-dibenzo (b,e)-1,4-dithiepin and in the case of the both possible combinations of atoms of oxygen and sulfur we are dealing with derivatives of 6H-dibenz(b,e)-1,4-oxathiepin and 11H- dibenz(b,f)-1,4-oxathiepin. Compounds according to the invention contain in molecules various types of aminoalkyl groups connected to the single carbon atom of the central ring which may be considered (dimethylaminomethyl, 2- dimethylaminoethyl, 2-methylaminoethyl, 3-dimethylaminopropyl, 3-methylaminopropyl, 3-piperidinopropyl, 1-methyl-3-piperidyl- methyl, 1-methyl 4-piperidyl. Some of the compounds according to the invention are substituted in the benzene rings with atoms of halogens, with methoxyl, trifluoromethyl, trifluoro- methylthio group. The invention includes not only the bases but also their salts with pharmaceutically acceptable acids. The invention includes also several methods for the prepara- tion of the compounds defined consisting in (a) construction of the whole molecules by cyclization of the diaryl ether or diaryl sulfide derivatives with a preformed side chain, (b) introduction of the side chains into the first synthesized tricyclic systems, (c) modification of the side chains in the amino group fragment, (d) selective oxidations to N-oxides, sulfoxides or sulfones. The compounds of the invention have mild or very intensive psychotropic activity and in agreement with their structures they are neuroleptics, tranquillizers and antidepressants.

398212

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