C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 281/02 (2006.01) C07D 281/10 (2006.01) C07D 417/12 (2006.01)
Patent
CA 2158223
A method for the preparation of 3-hydroxy-5-[2- (dimethylamino)-eth yl]-2,3-dihydro-4-(methoxyphenyl)-1,5- benzothiazepin-4(5H)-one and use of the product prepared by this method for making pharmaceutical compositions and pharmaceutically active compounds is disclosed starting with N-alkylation of 3-hydroxy-2,3-dihydro-4- (methoxyphenyl)-1,5-benzothiazepin-4(5H)-one with a (dimethylamino)ethyl halide wherein the N-alkylation reaction is carried out in a reaction mixture comprising 2-butanone and water. The product of this reaction and its salts have utility as pharmaceutically active compounds and as intermediates for making pharmaceutically active compounds. The disclosed method and use is simpler, more efficient and safer than prior known methods and produces a product of superior purity.
Fetherstonhaugh & Co.
Orion Corporation Fermion
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