| 摘要 |
PURPOSE:To obtain the title compound readily by reaction of d-cis-2,3-dihydro-3 hydroxy-2-(4-methoxyphenyl)-1,5-henzothiazepin-4-(5H)-one with 2-chloro-N,N- dimethylethylamine in the presence of a specific compound. CONSTITUTION:The reaction of the compound of formula I with another compound of formula II or its hydrochloride is carried out in a reaction medium such as acetonitrile or 1,2-dimethoxyethane, in the presence of (1) potassium fluoride, (2) gamma-alumina, (3) free water, or water from crystalline water of the potassium fluoride or adsorption water to the alumina, when needed, in the coexistence of a basic compound other than potassium fluoride, preferably at about 50 deg.C for 2-6hours to give d-cis-5-[2-(dimethylamino)-ethyl]-2,3-dihydro-3- hydroxy-2-(4-methoxyphenyl]-1,5-benzothiazepin-4(5H)-one of formula III. |
