| 摘要 |
PURPOSE:To introduce dimethylaminoethyl group into d-cis-3-OH-2,3-dihydro-2-(4- methoxyphenyl)-1,5-benzothiazepin-4(5H)-one, by reacting the compound with 2-Cl-N,N-dimethylethylamine. CONSTITUTION:The objective compound of formula II can be produced in one step at a stroke in high purity and yield, by reacting the compound of formula I with the compound of formula II in an aprotic solvent in the presence of KF-Al2O3 at 20-30 deg.C. The amount of KF-Al2O3 is 2-5 times equivalent (in terms of KF) based on the compound of formula I and the content of KF in KF-Al2O3 is usually 40wt.%. The compound of formula III is useful e.g. as a synthetic intermediate for diltiazem hydrochloride which is a drug having coronary vasodilating action. |
