PREPARING AMIDINES DERIVED FROM 6-HYDROXY-2,5,7,8-TETRAMETHYLCHROMANE-2-CARBOXYLIC ACID

摘要

The invention concerns the use of novel intermediates of general formula (II)B defined below for the synthesis of amidines derived from (-)-6-hydroxy-2,5,7,8 tetramethylchromane-2-carboxylic acid, such as for example, (S)-N-{4-[4-(3,4-dihydro-6-hydroxy-2,5,7,8-tetramethyl-2H-1-benzopyran-2-yl)-carbonyl]-1-piperazinyl]phenyl}-2-thiophenecarboximidamide. In general formula (II)B: A' represents the radical (a), X represents -Z1-CO-; rho represents a bond or a heterocycle selected among the group consisting of piperidine, piperazine, homopiperazine, 2-methylpiperazine, 2,5-dimethyl-piperazine, 4-aminopiperidine radicals; Y represents a radical selected among the -Z2- and -NR3-Z2 radicals; R3 represents a hydrogen atom, a linear or branched alkyl radical with 1 to 6 carbon atoms or a -COR4 radical; R4 represents a linear or branched alkyl radical with 1 to 6 carbon atoms; Z1 and Z2 independently represent a single bond or a linear or branched alkyl radical with 1 to 6 carbon atoms; and R6 represents a hydrogen atom or a OH group.