PROCESS FOR THE PREPARATION OF 1-2(-PYRIMIDINYL)-PIPERAZINE

摘要

This method finds application in obtaining high-purity 1-/2-pyrimidinyl/-piperazine for use as a starting material in the synthesis of Buspyrone, a tranquilliser with an anxiolytic effect. The method allows obtaining high-purity 1-/2-pyrimidinyl/-piperazine at high yield rates thus creating optimal conditions for the synthesis of the final product. The method involves reacting equimolar amounts of N-nitroso piperazine and 2-chloropyrimidine in a triethylamine medium at temperatures not exceeding 95 degrees C. The resulting 1-/2-pyrimidinyl/-4-nitroso piperazine is boiled in a mixture of hydrochloric acid and lower alkyl alcohol whereby the nitroso group hydrolyses and the product settles in the form of dihydrochloride.