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US 5,495,013 AGranted
Process for the preparation of Diltiazem
AssigneeProfarmaco Nobel S.r.l.
InventorsFulvio L. Piselli, Piermarino Boschi, Claudio Navoni
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Abstract
A process for the preparation of Diltiazem of formula (I) ##STR1## starting from the corresponding benzothiazepine and carried out throughout a 11 the steps in a single solvent.
Claims3
A process for the preparation of (+)cis-3-acetoxy-5-2,3-dihydro-2 -(4-methoxy-phenyl)-1,5-benzothiazepin-4-(5H)-one of formula (I):
- ##STR5## and a salt thereof, which consists of the following steps:
- a) reacting under anhydrous conditions (+)-cis-3-hydroxy-2,3-dihydro-(4-methoxyphenyl)-1,5-benzothiazepin-4-(5H)- one of fomula (II):
- ##STR6## with 2-dimethylaminoethyl chloride of formula (III):
- (CH.sub.3).sub.2 N-CH.sub.2 CH.sub.2 -C1 (III)
- in the presence of sodium carbonate, to give (+)-cis-3-hydroxy-5-2,3-dihydro-2-(4-methoxyphenyl) -1,5-benzothiazepin-4-(5H)-one of formula (IV):
- ##STR7## b) acetylating said compound of formula (IV);
- c) recovering said compound (+)-cis-3-acetoxy-5-2,3-dihydro-2-(4-methoxyphenyl) 1,5-benzothiazepin-4-(5H)-one of formula (I) and when a salt thereof is desired, adding an acid to form the salt of said compound of formula I, wherein all said steps a) -c) are carried out in an aromatic solvent which is a member selected from the group consisting of toluene, xylene, chlorobenzene and dichlorobenzene.
4 more elements
Dependencies are inferred from the claim text.