GB763044A - Pteridin derivatives - Google Patents

Abstract

The invention comprises pteridin derivatives of the formula <FORM:0763044/IV(b)/1> wherein X and X1 stand for alkyl and Y and Y1 stand for hydrogen or alkyl, or X and Y or X1 and Y1 may be joined with the adjacent nitrogen atom to form a heterocyclic ring, and wherein of R and R1, one stands for hydrogen or a phenyl group which may be substituted by halogen or by an alkoxy group of not more than four carbon atoms and the other stands for a phenyl group, which may be substituted by halogen or by an alkoxy group of not more than four carbon atoms. They are prepared (a) by heating a compound of the formula <FORM:0763044/IV(b)/2> (see Specification 763,120) with an a -diketone R.CO.CO.R1 or an oxime or phenylhydrazone thereof; or (b) by oxidizing the corresponding 7,8-dihydropteridins such as those described in Specification 763,138. In examples: (1) 2,4-bismethylamino - 5,6 - diaminopyrimidine is heated with benzil to give 2,4-bismethylamino6,7 - diphenylpteridin; (2) to (4) by similar processes there are obtained the 2-methylamino - 4 - dimethylamino -, 2 - dimethylamino - 4 - methylamino -, and 2,4 - bisdimethylamino - 6,7 - diphenylpteridin; (5) 2,4bismethylamino - 5,6 - diaminopyrimidine sulphate is heated with anisil to give 2,4-bis-methylamino - 6,7 - di - p - methoxyphenylpteridin; (6) 2,4 - bisdimethylamino - 6,7 - diphenyl - 7,8 - dihydropteridin is oxidized with potassium permanganate to 2,4-bisdimethylamino - 6,7 - diphenylpteridin; (7) 2,4 - bisdimethylamino - 5,6 - diaminopyrimidine sulphate is heated with phenylglyoxal hydrate and sodium acetate in ethanol to give 2,4-bis-dimethylamino - 7 - phenylpteridin; (8) 2,4bisdimethylamino - 5,6 - diaminopyrimidine sulphate is heated with phenylglyoxal hydrate and sulphuric acid in ethanol to give 2,4-bisdimethylamino - 6 - phenylpteridin; and (9) 7 - p - chlorophenyl - 2 - dimethylamino - 4methylamino - 6 - phenyl - 7,8 - dihydropteridin is oxidized with potassium permanganate to 7p - chlorophenyl - 2 - dimethylamino - 4 - methylamino - 6 - phenylpteridin. Other specific products of the first general formula above are described including those in which -NXY is ethylamino, diethylamino or piperidino, -NX1Y1 is ethylamino, diethylamino, isopropylamino, n-butylamino, n-propylamino, piperidino or morpholino, and R or R1 are 5-, m- or p-chlorophenyl. According to the Provisional Specification R and R1 may be hydrogen or hydrocarbon or substituted hydrocarbon radicals.