Analogifremgangsmåde til fremstilling af phenthiazinderivater eller alkalimetal-, jordalkalimetal-, ammonium- eller aminsalte deraf.

摘要

Compounds of the general formula wherein R is H or a menthyl group, R1 or a methyl or ethyl group and Y is H or a halogen atom, or an alkyl, alkoxy or alkylthio group of 1-4 carbon atoms, R being methyl when R1 and Y are both H, and their salts are prepared by subjecting a compound of the formula to the Willgerodt reaction or Kindler modification of it and hydrolysing the resulting amide or thioamide or by hydrolysing and decarboxylating a compound of the formula wherein R2 and R3 each are an alkyl group of 1-4 carbon atoms and R11 is a methyl or ethyl group, or by hydrolysing a compound of the formula where T is a radical capable of conversion to a carboxyl group by hydrolysis. The following starting materials and intermediates are also prepared: (10-methyl-3phenothiazinyl)-, (10 - methyl - 7 - methoxy - 3phenothiazinyl)-, (7,10 - dimethyl - 3 - phenothiazinyl)-, (7 - chloro - 3 - phenothiazinyl)and (7 - methoxy - 3 - phenothiazinyl) - acetothiomorpholide; 3 - acetyl - 7 - methoxy - 10 methyl-, 3 acetyl - 7, 10 - dimethyl-, 3 - acetyl- 7chloro-, 3 - acetyl - 7 - methoxy- and 3,10 - diacetyl - 7 - chloro - phenothiazine; 2 - amino - 4acetyl - 21 - bromo - 51 - methoxy-, 2 - amino - 4acetyl - 21 - bromo1 - 51 - methyl-, 2 - nitro - 4acetyl - 5 methoxy- and 2 - nitro - 4 - acetyl - 21bromo - 51 - methyl - diphenylsulphides; 2 -bromo5 - methoxythiophenol; methyl ethyl methyl(3 - phenothiazinyl) - malonate; methyl ethyl(3 - phenothiazinyl) - malonate; methyl ethyl methyl - (10 - methyl - 3 - phenothiazinyl)malonate; methyl ethyl - (10 - methyl - 3 - phenothiazinyl) - malonate; methyl ethyl ethyl(10 - methyl - phenothiazinyl) - malonate; methyl ethyl - (7 - methoxy - 10 - methyl - 3 - phenothiazinyl) - malonate; methyl ethyl methyl(7 - methoxy - 10 - methyl - 3 - phenothiazinyl) - malonate; ethyl - 3 - (3 - phenothiazinyl) - 3-methoxy - carbonyl - 2 - oxopropionate; methyl - (10 - methyl - 3 - phenothiazinyl) - acetate; methyl - (7 - methoxy - 10 - methyl - 3 - phenothiazinyl) - acetate; (10 - methyl - 3 - phenothiazinyl) - acetonitrile; 3 - bromomethyl- and 3 - hydroxymethyl - 10 - methyl - phenothiazine. Pharmaceutical compositions useful as anti-inflammatory agents comprise the compounds of the invention and a carrier therefor. The compositions are in forms suitable for oral, parenteral and rectal administration.