ES351389A1 - Procedure for the obtaining of basically substituted heterocicles. (Machine-translation by Google Translate, not legally binding) - Google Patents

Abstract

Procedure for obtaining basically substituted heterocycles, especially dibenzo [b, f] -1,4-oxazepines, dibenzo [b, f] -1,4-thiazepine and dibenzo [b, e] -1,4-diazepines 11- basically substituted for the general formula: **(See formula)** where Z means an oxygen atom, a sulfur atom, a sulfinyl group or an imino group; R1 representing a hydrogen atom, an alkyl or hydroxyalkyl group containing at most three C atoms, or an alkoxy-alkyl or alkoyloxyalkyl group containing a maximum of six C atoms; R2 representing a nitro group, an amino group, an aminosulfonyl group of the formula -SO2NR3R4, in which R3 and R4 are the same or different and represent hydrogen atoms or methyl groups, an alkylsulfinyl group of the formula -SOR5, or a alkylsulfonyl group of the formula -SO2R5, where R5 is an alkyl group containing a maximum of three C atoms; as well as acid addition salts thereof; characterized by: a) a compound of the formula is reacted; **(See formula)** where Z and R2 have the same meaning mentioned and X represents a hydrogen-separable moiety of amines with piperazine, respectively a piperazine derivative of the formula **(See formula)** where R1 has the aforementioned meaning, or because b) Acid amides or thioamides of the formula are condensed intramolecularly **(See formula)** where Z, R1 and R2 have the aforementioned meaning, and Y represents an oxygen or sulfur atom, or because c) for the representation of products, in which Z represents an oxygen or sulfur atom, urea derivatives of the formula are dehydrated: **(See formula)** where R1 and R2 have the mentioned meaning, or because; d) for the preparation of the desired products, with the exception of the compounds, in which R2 signifies an amino group, amidines of the formula are treated: **(See formula)** where Z has the aforementioned meaning and R'2 has one of the meanings of R2, with the exception of those of the amino group, with a reactable ester of an alcohol of the formula: **(See formula)** where R1 has the aforementioned meaning, or because e) for the preparation of compounds, in which R2 represents an amino group, corresponding nitro compounds are reduced, or because f) for the preparation of compounds, in which Z means a sulfinyl group, corresponding compounds are oxidized, in which Z represents a sulfur atom, or because: g) for the preparation of compounds, in which R2 represents a group of alkylsulfinyl or alkylsulfonyl, corresponding thioalkyl compounds are treated with a moderate, respectively strong, oxidation medium, or for the preparation of compounds, in which it represents a group of alkylsulfonyl, corresponding compounds are treated with an alkylsulfinyl group with a strong oxidation medium, or because finally h) for the preparation of compounds, in which R2 represents an aminosulfonyl group, corresponding compounds are reacted which, instead of the aminosulfonyl group, have a -SO2X group, in which X represents a moiety, separable with hydrogen, of amines, with ammonia, respectively an amine of the formula HNR3R4, in which R3 and R4 have the aforementioned meaning, optionally with subsequent introduction of a non-hydrogen substituent R1, in products, in which R1 represents hydrogen, and/or with subsequent affiliation of a hydroxyalkyl group R1, after which the obtained reaction products are isolated as free bases or in the form of their acid addition salts, with suitable inorganic or organic acids. (Machine-translation by Google Translate, not legally binding)