2-Pyrimidinamine, N-(1-methylethyl)- (9CI)

Originator

Nerfactor,Ipsen,France,1981

The Uses of 2-Pyrimidinamine, N-(1-methylethyl)- (9CI)

Isaxonine is a neurotropic agent. Isaxonine prevents synaptic remodeling by suppression of the redundant nerve endings from additional axons. Isaxonine is transformed by cytochrome P 450 into reactive metabolites that lead to immunoallergic hepatitis in man.

Definition

ChEBI: Isaxonine is an aminopyrimidine.

Manufacturing Process

6 liters of ethanol and 685 g (5 mold of 2-isopropylamino pyrimidine were added to a 10 liter reactor and stirred. To the solution were added 600 g (5.2 mols) of phosphoric acid and the mixture was boiled under reflux for one hour. There was obtained a dark green solution which was treated with 30 g of carbon black. After separation and crystallization while stirring overnight, the crystallized product was separated, washed with ethanol and dried at 50°C. There was obtained 1,027 g (87% yield) of a white powder melting at 125°C. The analysis of the compound showed a good correspondence with the formula C7H14O4N3P.

brand name

Nerfactor;Verfactor.

Therapeutic Function

Neurotropic

World Health Organization (WHO)

Isaxonine phosphate was introduced in 1981 and marketed exclusively in France for the treatment of peripheral neuropathy. In January 1983 indications for use were restricted following its association with cases of toxic hepatitis. It was subsequently withdrawn in June 1983.