ES398223A1 - A procedure for the preparation of benzodiacepine derivatives. (Machine-translation by Google Translate, not legally binding) - Google Patents

Abstract

A procedure for the preparation of benzodiazepine derivatives of the general formula **(See formula)** in which B represents methylene (-CH2-) or carbonyl (-CO-); R1, R2, R3 and R4 represent hydrogen or lower alkyl, R5 represents hydrogen or halogen and R6 and R7 represent hydrogen or taken together an additional C-N bond, and its pharmaceutically acceptable acid addition salts, the process of which comprises a) to prepare compounds of the formula I, where R1 represents hydrogen, reduce a compound of the general formula **(See formula)** where B, R2, R3, R4, R5, R6 and R7 have the above meaning, or b) to prepare compounds of formula I, where R2 represents lower alkyl, provided that when B is carbonyl R3 is hydrogen, treat a compound of formula II above with the provision that when B is carbonyl, R3 is hydrogen, with a lower lithiumalkyl compound, or c) to prepare compounds of formula I, where B represents carbonyl and R6 and R7 taken together, represent an additional C-N bond, cyclizing a compound of the general formula **(See formula)** in which R1, R2, R3, R4 and R5 have the above significance, or d) to prepare compounds of formula X, where R3 represents lower alkyl, 1-properly alkylating a compound of the general formula **(See formula)** in which B, R1, R2, R3, R4, R5, R6 and R7 have the above significance, or e) to prepare compounds of formula I, where R6 and R7 taken together represent an additional C-N bond to oxidize a compound of the general formula **(See formula)** in which B, R1, R2, R3, R4, and R5 have the above significance, or f) to prepare compounds of the above formula Ib, reduce a compound of the general formula **(See formula)** in which B, R1, R2, R3, R4 and R5 have the above significance, or, g) to prepare compounds of formula I, where B represents methylene and R6 and R7 represent hydrogen, reduce a compound of the general formula **(See formula)** in which R1, R2, R3, R4 and R5 have the above significance, and h) if desired, converting a obtained compound into a pharmaceutically acceptable acid addition salt. (Machine-translation by Google Translate, not legally binding)