摘要:
Citalopram can be industrially and economically produced and at a high yield by reacting a compound of the following formula [VI] with 3-(dimethylamino)propyl chloride in the presence of at least one of N,N,N',N'-tetramethylethylenediamine and 1,3-dimethyl-2-imidazolidinone and a condensing agent. The compound of the following formula [III], which is a key compound for the production of citalopram, can be easily produced by subjecting the compound of the following formula [II] to reduction and cyclization.
摘要:
A process for producing L-valine benzyl ester p-toluenesulfonate which involves the steps of reacting L-valine with benzyl alcohol in at least one aromatic solvent selected from among toluene, monochlorobenzene and xylene in the presence of p-toluenesulfonic acid under azeotropic dehydration conditions and crystallizing L-valine benzyl ester p-toluenesulfonate from the liquid reaction mixture thus obtained. Use of this process makes it possible to safely, conveniently and industrially advantageously produce L-valine benzyl ester p-toluenesulfonate which is appropriately usable as an intermediate of drugs such as remedies for hypertension.
摘要:
A pyridinemethanol compound is an important intermediate for a mirtazapine which is useful as an antidepressant. The pyridinemethanol compound is obtained by reducing potassium pyridinecarboxylate represented by the formula (I): with a metal hydride.
摘要:
A method for producing camphorsultam, which includes the following steps 1 to 4:
Step 1: reacting camphorsulfonic acid with a halogenation agent to give camphorsulfonyl halide, Step 2: reacting the camphorsulfonyl halide with ammonia to give camphorsulfonamide, Step 3: subjecting the camphorsulfonamide to dehydration and ring closure to give camphorsulfonimine, and Step 4: reducing the camphorsulfonimine with sodium borohydride in an aqueous isopropanol solution. According to this invention, camphorsultam and intermediates thereof can be obtained by an industrial method which is comparatively safe to the environment and human body, economical, and which is simple and easy.
摘要:
Citalopram can be industrially and economically produced and at a high yield by reacting a compound of the following formula [VI] with 3-(dimethylamino)propyl chloride in the presence of at least one of N,N,N',N'-tetramethylethylenediamine and 1,3-dimethyl-2-imidazolidinone and a condensing agent. The compound of the following formula [III], which is a key compound for the production of citalopram, can be easily produced by subjecting the compound of the following formula [II] to reduction and cyclization.