Patent ID: 7569690
Filing Date: 2009-08-04
Classification: C07D

Abstract:
1. A process for producing an oxycarbonyl-substituted piperazine derivative comprising oxycarbonylating a piperazine derivative represented by formula (1) in the presence of 1) a reagent comprising benzyl chlorocarbonate or di-tert-butyl dicarbonate and an organic alcohol solvent with a water content of 15 wt % or less to produce an oxycarbonyl-substituted piperazine derivative represented by formula (2) wherein the R 1 in the formula (1) and the formula (2) denotes a methyl group, and R 2 , R 3 and R 4 denote a hydrogen atom respectively; X denotes a tert-butyl group or benzyl group; and the compounds represented by the formula (1) and the formula (2) are optically active substances, and 2) at least one compound selected from the group consisting of pyridine, α-picoline, β-picoline, γ-picoline, 2-ethylpyridine, 3-ethylpyridine, 4-ethylpyridine, 2-n-propylpyridine, 3 -n-propylpyridine, 4-n-propylpyridine, 2-isopropylpyridine, 2-phenylpyridine, 2-vinylpyridine, 3-aminopyridine, 2-hydroxypyridine, 2-methoxypyridine, 2-chloropyrodine, 3-fluoropyridine, 4-bromopyridine, 3-iodopyridine, 2-formylpyridine, 3 -acetylpyridine, 2-pyridinecarboxylic acid, methyl 3-pyridinecarboxylate, 3 -pyridinecarboxylic acid amide, 2-cyanopyridine, 3 -nitropyridine, pyrrole, indole, pyrazole, isoxazole, isothiazole, indazole, imidazole, oxazole, thiazole, benzimidazole, quinoline, isoquinoline, pyridazine, pyrimidine, pyrazine, quinoxaline, carbazole, α-aminonaphthalene, β-aminonaphthalene, aniline, 2.6-lutidine and trimethylamine.