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) γ-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°C for 2W6hours 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.
ISHIZUKA NORIYASU
FUTSUKAICHI OSAMU
OHIRA YUTAKA
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