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US 7,002,008 B2Granted
Process for the preparation of 1-(4-fluorophenyl)-4(S)-(4-hydroxyphenyl)-azetidin-2-one
OwnerBomi Patel Framrozeinventor
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Abstract
A process for preparing a compound of the formula comprising: (a) formation of 3(S)-(4-hydroxyphenyl)-3-methanesulfonyloxy-propionic acid methyl ester compound of the formula (b) cyclization of the product of Step (a) with 4-fluoroaniline to yield 1-(4-fluorophenyl)-4(S)-(4-hydroxyphenyl)-azetidin-2-one.
Claims11
A compound of formula III and
- chemical name 3(S)-(4-hydroxyphenyl)-3-methanesulfonyloxy-propionic acid methyl ester.
A process for preparing a compound of formula I comprising:
- (a) resolving racemic 3-(4-hydroxyphenyl)-3-hydroxy-propionic acid into 3(R)-(4-hydroxyphenyl)-3-hydroxy-propionic acid and 3(S)-(4-hydroxyphenyl)-3-hydroxy-propionic acid;
- (b) making 3(S)-(4-hydroxyphenyl)-3-hydroxy-propionic acid methyl ester from 3(S)-(4-hydroxyphenyl)-3-hydroxy-propionic acid;
- (c) forming 3(S)-(4-hydroxyphenyl)-3-methanesulfonyloxy-propionic acid methyl ester by contacting 3(S)-(4-hydroxyphenyl)-3-hydroxy-propionic acid methyl ester with methane sulfonyl chloride;
- (d) reacting 3(S)-(4-hydroxyphenyl)-3-methanesulfonyloxy-propionic acid methyl ester with 4-fluoroaniline in the presence of alkali halide to form the compound of formula I.
1 more element
Dependencies are inferred from the claim text.