PRODUCTION OF 1,2-DISUBSTITUTED-3-NITROISOTHIOUREA COMPOUND

PROBLEM TO BE SOLVED: To produce the subject compound useful as an important intermediate for pharmaceuticals and agrochemicals in one step by reacting a nitroisothiourea compound with an alkylation agent in various organic solvents in the presence of a base. SOLUTION: The objective 1,2-disubstituted-3-nitroisothiourea compound of the formula II (R2 is a 1-4C alkyl) can be produced by reacting (A) a nitroisothiourea compound of the formula I (R1 is an alkyl, phenyl or a 5- or 6-membered heterocyclic group containing at least one of N, O and S) with (B) an alkylation agent selected from an alkyl halide and a dialkyl sulfate in the presence of (C) a base in (D) an organic solvent. For example, 1,2 dimethyl-3-nitroisothiourea is produced by using 2-methyl-3-nitroisothiourea as the component A, dimethyl sulfate as the component B, potassium carbonate as the component C and DMI as the component D.