Tetrahydrofuran → HCID 86673126, compound

Participants

Reaction Steps

In accordance with Scheme 1 below, ethyl 4-chloro-2-methylthiopyridine-5-carboxylate (II with A=CH) (prepared according to Todd et al., J. Amer. Chem. Soc. (1943), 65, 350-354; Pesson, M., Eur. J. Med. Chem. (1974), 9(6), 585-590; Shadbolt, R., J. Chem. Soc. (1967), 13, 1172-1178) or ethyl 4-chloro-6-methyl-2-methylthiopyridine-5-carboxylate (II with A=C-Me) (prepared according to the method described in WO 2005/105 801) is reacted with an amine of formula R5—NH2 (in which R5 is as defined previously in relation to formula (I) according to the invention) in an organic solvent such as THF or dioxane, and in the presence of an organic base, for example triethylamine, at room temperature, according to the method described by D. Boschelli et al. in J. Med. Chem. (1998), 41, 4365-4377, to give an ethyl 4-amino-2-methylthiopyridine-5-carboxylate derivative of formula (III).

Provenance & Evidence