| 摘要 |
The invention comprises compounds of the general formula <FORM:0980853/C2/1> and their acid addition salts and guaternary ammonium derivatives (wherein Z represents S, SO or -(NR1)-, whereR1 is H or a protecting group (e.g. an acyl orbenzyl group), or a C1 to C5 alkyl or C2 to C5 alkenyl group; R2 and R3 may be the same or different and represent hydrogen atoms or alkyl, alkenyl, amino, mono- or dialkylamino or mono- or di-alkylaminoalkyl groups, or monocyclic aryl or aralkyl groups, which aryl and aralkyl groups may be substituted by halogen atoms or trifluoromethyl, hydroxy, alkyl, or C1 to C3 alkoxy or alkylmercapto groups, or R2/t and R3 together with the nitrogen atom may form a cycloalkylamino group which may contain further heteroatoms, which heteroatoms, if nitrogen, may carry hydrogen atoms or alkyl, hydroxyalkyl or alkoxyalkyl groups; and R4 and R5 represent hydrogen or halogen atoms or trifluoromethyl, hydroxy or C1 to C3 alkyl, alkoxy or alkylmercapto groups), and the preparation thereof by reacting a compound of formula <FORM:0980853/C2/2> (wherein R1 may not be H) with a dehydrating agent, or by reacting a compound of formula <FORM:0980853/C2/3> (wherein A represents a halogen atom or a C1 to C3 alkoxy or alkylthio group) with a compound of formula <FORM:0980853/C2/4> and, if desired, converting the products into acid addition salts or quaternary ammonium compounds. Compounds in which Z is SO can also be obtained by oxidizing the thiazepine compounds (Z=S). The products are useful as analgesics, chemotherapeutic agents, antihistaminics, or antiphlogistic or antioedemic agents. Ureas of the second general formula above are obtained by reacting suitable o-amino-diphenylamines or o-amino-diphenyl sulphides with potassium cyanate, or with phosgene or chlorocarbamate followed by reaction with an amine of formula R2-NH-R3. Dibenzodiazepines and dibenzothiazepines of the third general formula above are obtained by thermal cyclization of suitable o-amino-diphenylamine - o1 - carboxylic acids or o - amino-o1-carboxydipheny sulphides to form the lactam, and then reacting the lactam with phosphorus pentasulphide and then with alkali and dialkyl sulphate, or reacting the lactam with phosphorus oxychloride and phosphorus pentachloride. |
