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US 2014/0200342 A1Published application
Process for preparing 3'-thiosubstituted cephalosporins employing a pencillin g acylase
AssigneeDSM Sinochem Pharmaceuticals Netherlands B.V.
InventorsHarold Moody, Claudia Cusan, Gerard Ijpeij
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Abstract
The present invention relates to a process for the preparation of 3′-thiosubstituted cephalosporins by enzymatic condensation of a nucleus with a phenylglycine derivative. Furthermore the present invention relates to a crystalline form of a compound of general formula (1) wherein R2 is OH and X is S and R1 is a radical of formula (2a) with R3 is CH3.
Claims12
A process for the preparation of a compound of general formula (1)
- wherein R1 is a radical of formula (2a), (2b), (2c), (2d), (2e) or (2d) with R3 is CH3, CH2CO2H, CH2SO3H, CH2CH2OH or CH2CH2N(CH3)2 and R4 is hydrogen or CH3
- and wherein R2 is H or OH and X is CH2, O or S, characterized in that a compound of general formula (3) or a salt thereof wherein R1 and X are as defined above
- is mixed with D-4-hydroxyphenylglycine amide or an ester of D-4-hydroxyphenylglycine or D-phenylglycine amide or an ester of D-phenylglycine in the presence of a penicillin G acylase.
A crystalline form of a compound of general formula (1)
- wherein R1 is a radical of formula (2a)
- with R3 is CH3 and wherein R2 is OH and X is S, characterized in that said crystalline form of a said compound of general formula (1) has an XRD spectrum with peaks at 2θ values of 13.9±0.3, 19.1±0.3, 28.1±0.3, 32.2±0.3 and 33.9±0.3.
Dependencies are inferred from the claim text.