Synthetic intermediate for epothilone derivative and production method thereof
AssigneeSumika Fine Chemicals Co., Ltd.
InventorsMitsuhiro Iwasaki, Kiyoshi Sugi, Hideto Miyamoto, Nobushige Itaya
Life of this patent
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Abstract
The β-keto ester compound, β-hydroxy acid compound and acetonide form of a 1,3-diol derivative of the formulas (I), (V) and (VIII) 1 wherein each symbol is as defined in the specification, are useful as a synthetic intermediate for an epothilone derivative being developed as a pharmaceutical agent having an antitumor activity.
Claims28
A β-keto ester compound represented by the following formula
- 65
- wherein R4 is hydrogen atom or alkyl group having 1 to 6 carbon atoms, or an optically active form thereof.
A β-hydroxy acid compound represented by the following formula
- 69
- wherein R2 is hydrogen atom or alkyl group having 1 to 6 carbon atoms, and R4 is hydrogen atom or alkyl group having 1 to 6 carbon atoms, provided that when R4 is alkyl group having 1 to 6 carbon atoms, R2 should be tert-butyl group, an optically active form thereof or a salt thereof.
An acetonide form of a 1,3-diol derivative, which is represented by the following formula
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- or an optically active form thereof.
A production method of a 1,3-diol derivative represented by the following formula
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- or an optically active form thereof, which comprises reducing a β-hydroxy acid compound represented by the following formula
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- wherein R2 is hydrogen atom or alkyl group having 1 to 6 carbon atoms, or an optically active form thereof.
Dependencies are inferred from the claim text.