To selectively obtain a alkylnitroguanidine in one step useful for organic intermediates, medicines, agrochemicals, especially penetrative insecticides by alkylating nitroguanidine derivatives with an alkylating agent.
According to this method 2-nitroguanidine derivatives of formula II (R is an 1-4C alkyl) are capable of obtaining by alkylation of (A) nitroguanidine derivatives of formula I (A is a (substituted) heterocyclic ring or phenyl) in the presence of a base or an acid and base, in a solvent by an alkylating agent (preferably an 1-4C dialkylsulfuric acid). For example, 1- methyl-2-nitro-3-[(tetrahydro-3-franyl)methyl]guanidine is obtained by carrying out the reaction using 3-tetrahydrofurylmethylnitroguanidine as component A and dimethyl sulfuric acid as component B in the presence of sodium hydroxide, in dimethylformamide as solvent.
NAGAHARA KIYOTERU
MATSUNO YUUSEN
ODAKA KENJI
