NEW MATERIAL:dl-cis-2-( 4-Methocyphenyl ) -3-hydroxy-5-[ N, N-dimethylborane (B-N)-aminoalkyl]-2,3-dihydro-1,5-benzothiazepin-4(5H)-one of formula I (n is 1W5).
USE: Synthetic intermediate of antinicotinic agent, blood platelet coagulation inhibitor, antibacterial agent, and coronary vasodilator.
PROCESS: The compound of formula I can be prepared by reacting 2-(4-methoxyphenyl)-5-dimethylaminoalkyl-2,3-dihydro-1,5-benzothiazepin-3,4(5H)-dione of formula II or its acid addition salt with a borohydride compound. The compound of formula II used as a raw material is also a novel substance, and can be prepared by the reaction of 2-(4-methoxyphenylmethylidene)-4-dimethylaminoalkyl-2H-1,4-benzothiazin-3(4H)-one with trimethyl halogenosilane, hydrogen peroxide, and water.
MITSUMORI NAOMICHI
SASAO YASUTAKA
UNEDA TAKASHI
TAKATANI MASAHIRO
