Heteroaryl acetonitrile preparation in high yield, for use as intermediate for agrochemicals or drugs, from heteroarylium salt and finely divided alkali metal cyanide in organic solvent

摘要

Preparation of heteroaryl acetonitriles (I) involves reacting a heteroarylium salt (II) with a mixture of an alkali metal cyanide (III), at least 50 wt. % of which has a particle size of 1000 mum or less, and an organic solvent. Preparation of heteroaryl acetonitriles of formula Het-(CH2CN)n (I) involves reacting a heteroarylium salt of formula Het-(CH2X)n . (HY)m (II) with a mixture of an alkali metal cyanide (III), at least 50 wt. % of which has a particle size of 1000 mum or less, and an organic solvent. n = 1 or 2; Het = optionally mono- or polysubstituted mono-, bi- or tricyclic, 5-18 membered heteroaryl, where each ring contains 0-3 heteroatoms and Het overall contains 1-5 heteroatoms selected from O, S and N, provided that at least one N heteroatom is present; X = Cl, Br, I or OSO2R1; R1 = 1-12C alkyl, 1-12C perfluoroalkyl or 6-14C aryl; Y = anion of an acid.