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US 6,184,380 B2Granted
Process for preparing naphthyridones and intermediates
AssigneePfizer Inc.
InventorsCharles K. Chiu, Lewin T. Wint
Life of this patent
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Abstract
A process for preparing a naphthyridone carboxylic acid and its derivatives makes use of side chain intermediates of formulae I and IV herein.
Claims7
A process for preparing a compound of the formula
- wherein
- R1 is benzyl, wherein the phenyl of the benzyl may be substituted by one or more of C1—C6 alkyl, C1—C6 alkoxy, halo, nitro, amino or trifluoromethyl, and
- R2 is C1—C6 alkyl, trifluoromethyl, or phenyl which may be substituted by one or more of C1—C6 alkyl, C1—C6 alkoxy, halo, nitro, amino or trifluoromethyl, which comprises
- (a) reducing a compound of the formula
- wherein R1 is as defined above, in the presence of iron and a organic solvent under acidic conditions, and
- (b) acylating the compound of formula III formed:
- with an acylating agent of the formula R2C(O)X wherein R2 is as defined above, and X is a leaving group.
4 more elements
Dependencies are inferred from the claim text.