| abstract |
3-(arylthiopropylamino)-1,5-aryloxathiepine derivatives (I) are new. 3-(arylthiopropylamino)-1,5-aryloxathiepine derivatives of formula (I) and their (hydrated) addition salts with (in)organic acids, tautomers, enantiomers and stereoisomers are new. R1 and R2 = H, fluoro, chloro, hydroxy, 1-3C alkyl, cyclopropyl, cyclopropoxy; or R1 +R2 = 5-membered non-aromatic ring, optionally including an oxygen atom; R3 = 1-3C alkyl, hydroxy or MeO; R4 = H or Me; and R5 and R6 = hydrogen, 1-3C alkyl, alkoxy or alkylthio, or alkylamino. Provided that when R4 is Me, the R5 is not alkyl, or OR4 and R5 complete a 5- or 6-membered ring containing at least one oxygen. Independent claims are also included for: (1) Methods for preparing (I); (2) Intermediate amines of formula (VI); (3) Method for preparing (I); (4) Aldehydes of formulae (II) and (V); and (5) Methods for preparing (II) and (V). R3 = 1-3C alkyl or MeO; and R4 = Me in (II) or methoxymethyl in (V). |