57521-63-8Relevant academic research and scientific papers
A new, general and regioselective method for the synthesis of 2,6-disubstituted 4-aminopteridines
Taghavi-Moghadam, Shahriyar,Pfleiderer, Wolfgang
, p. 6835 - 6836 (2007/10/03)
A new synthetic method for the preparation of 2,6-disubstituted 4-aminopteridines is described. Treatment of a-substituted 4,5,6-triaminopyrimidines with α-ketoaldoximes in MeOH affords in a regioselective one-step reaction 2,6-disubstituted 4-aminopteridines in high yield.
Process of preparing N[p-{[(2,4-diamino-6-pteridyl)-methyl]N10 -methylamino}-benzoyl]-glutamic acid
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, (2008/06/13)
A three-step process is provided for preparing the L,D and DL isomers of N[p-{[(2,4-diamino-6-pteridyl)-methyl]N10 -methylamino}-benzoyl]-glutamic acid. The first step produces: 2,4-diamino-6-hydroxymethyl pteridine by condensation in a buffered aqueous media of 2,3,4,5-tetraminopyrimidine dihydrochloride with the bisulphite addition product of 1,3-dihydroxyacetone in the presence of cysteine as catalyst and using selenium dioxide and a continuous air bubbling as oxidation agents. In the next step, 2,4-diamino-6-halomethylpteridine is obtained by halogenation of the previously obtained 2,4-diamino-6-hydroxymethylpteridine in an inert media with a halogenation agent such as thionyl chloride, in the presence of a basic catalyst such as pyridine or triethylamine. In the third step, N[p-{[(2,4-diamino-6-pteridyl)-methyl]-N10 -methylamino}-benzoyl-]-glutamic acid is produced by condensation of the 2,4-diamino-6-halomethylpteridine with N[p-(N-methylamino)-benzoyl]-glutamic acid at pH 3-4 in an aqueous buffered solution.
