ES314975A1 - A procedure for the preparation of fluorene i-oxides- (1,9-ef) -1,4-diazepine. (Machine-translation by Google Translate, not legally binding) - Google Patents

Abstract

A process for the preparation of 1-fluoreno- [1,9-ef] -1,4-diazepine oxides of the general formula: ** (See formula) ** wherein R3 and R5 represent hydrogen or a lower alkyl group, R4 represents hydrogen or a halogen, such as chlorine, the group being in position 5 or 7, R1 and R2, which may be identical or different, represent hydrogen or a lower alkyl containing from 1 to 6 carbon atoms, alkenyl, allyl, benzyl, alkylaryl hydroxyalkyl, amino, guanidino, furfuryl or a heterocyclic alkyl group, or R1 and R2 together with the adjacent nitrogen atom (1) form a dihydroxy group; -alcohilaminodialcohilamino, (2) a group of the formula (see formula), in which (see formula) is a nitrogenous heterocyclic group which may be substituted or (3) a heterocyclic group which may be substituted, such as an ethyleneimino group, morpholino, piperidino, pyrrolidino, hexamethyleneimino, n-methylpiperasino, n-beta-hydroxyethylpiperazino or -benzylpiperazine, as well as the acid addition salts of these compounds, in which process a compound of the general formula ** (See formula) ** wherein R3 and R5 represent hydrogen or a lower alkyl group, such as a methyl group, and R4 represents hydrogen or a halogen, such as chlorine, wherein R4 is at the 4 or 6 position and X represents a halogen such as chlorine or bromine, is reacted (1) with a primary amine or (2) with a nitrogen-containing heterocyclic compound different from morpholine in the presence of methanol, the compound obtained possibly being converted to an acid salt by a known method. (Machine-translation by Google Translate, not legally binding)