Synthesen auf dem Phenothiazin‐Gebiet. 4. Mitteilung. N‐substituierte Mercapto‐azaphenothiazin‐Derivate

Abstract

Im Rahmen unserer Untersuchungen uber Mercaptophenothiazin-Derivate I 2), die durch geeigncte Substitution am Ringstickstoff 3, zu pharmakologisch wirksamen Substanzen gefiihrt habcn, wurden durch entsprechende Synthese auch analoge Mercapto-azaphenothiazine I1 dargestellt. SUMMARYThe synthesis of a series of pharmacologically interesting N-substituted derivates of 6-methylmercapto-azaphenothiazine is described.Pharmazeutisch-chemisches Laboratorium SANDOZ, Base1

Neuropharmacological profile of 1-azaphenothiazine-10-thiolcarboxylates

“…Purified bases. 6 Unpurified bases. c Oxalates were analyzed for C, , N and hydrochlorides for N, S, Cl.…”

“…Compounds were administered iv in the following solvents: 1I20 (6, 10); 0.1 .Y HC1 (1, 8, 9); 15% v/v DMSO-HjO (5, 3, 7); 25% v/v polyethvleneglycol 300 (2); 25% v/v polyethylene glycol 200 (4). 6 Minimum dose at which reactive signs were observed in half of mice tested.…”

“…Maleate salts were pptd from Et20 solutions of the base. d Insol in all common solvents; leached with boiling EtOAe 6.…”