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US 2007/0185206 A1Published application
Method for preparing 15-keto-prostaglandin E derivative
AssigneeR-Tech Ueno, Ltd.
InventorsRyu Hirata, Tatsuya Matsukawa
Life of this patent
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Abstract
Disclosed is an improved method for preparing 15-keto-prostaglandin E derivative. According to the invention, the deprotection of protected hydroxy group required in manufacturing a 15-keto-prostaglandin derivative is conducted under the presence of a phosphoric acid compound.
Claims5
A. method for preparing a 15-keto-prostaglandin E derivative represented by formula (I):
- wherein,
- R1 is a saturated or unsaturated bivalent lower or medium aliphatic hydrocarbon residue, which unsubstituted or substituted with halogen, lower alkyl, hydroxy, oxo, aryl or heterocyclic, and at least one of carbon atom in the aliphatic hydrocarbon is optionally substituted by oxygen, nitrogen or sulfur;
- R2 is a saturated or unsaturated lower or medium aliphatic hydrocarbon, which is unsubstituted or substituted with lower alkyl, lower alkoxy, lower alkanoyloxy, cyclo(lower)alkyl, cyclo(lower)alkyloxy, aryl, aryloxy, heterocyclic or hetrocyclicoxy group;
- cyclo(lower) alkyl;
- cyclo(lower)alkyloxy;
- aryl;
- aryloxy;
- heterocyclic;
- or heterocyclicoxy group;
- B is —CH2—CH2—, —CH═CH— or —C≡C—;
- Q is —CH3, —COCH3, —OH, —COOH or a functional derivative thereof;
- X1 and X2 are hydrogen, lower alkyl, or halogen which comprises the step of hydrolyzing the compound represented by formula (II):
- wherein,
- A1 is a protecting group for hydroxy group, R1, R2, B, Q, X1 and X2 are the same as above in the presence of phosphoric acid compound.
11 more elements
Dependencies are inferred from the claim text.