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US 5,470,717 AGranted
Method for the preparation of certain .beta.-lactam antibiotics
AssigneeGist-Brocades N.V.
InventorKim Clausen
Life of this patent
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Abstract
The present invention relates to an improved method for the preparation of certain .beta.-lactam antibiotics by enzymatic acylation or by deprotection of a protected intermediate.
Claims11
A method of preparing a .beta.-lactam antibiotic comprising enzymatic acylation of a 7-amino-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene nucleus in water or in a mixture of water and one or more water-miscible organic solvents by enzymatic acylation with the acid or a derivative of the acid corresponding to the desired side chain, characterized in that naphthalene or a naphthalene derivative with the formula
- Naphthyl-R
- wherein Naphthyl- designates 1-naphthyl or 2-naphthyl and R is selected from the group consisting of hydrogen, halogen, hydroxy, nitro, cyano, branched or unbranched alkyl of 1 to 6 carbon atoms optionally substituted with cyano, branched or unbranched alkoxy of 1 to 6 carbon atoms and alkanoyl of 1 to 6 carbon atoms, where on a molar basis the ratio between the amount of naphthalene or naphthalene derivative present in the reaction mixture and the amount of .beta.-lactam antibiotic present in the reaction mixture is at least 0.45, is present in the reaction mixture during the formation of a naphthalene complex of the .beta.-lactam antibiotic which is isolated or decomposed to the .beta.-lactam antibiotic by deprotection of a protected intermediate.
Dependencies are inferred from the claim text.