| 摘要 |
The present invention relates to an improved process for the preparation of cefprozil DMF solvate of formula (I), which is useful for the preparation of cefprozil, comprising: i) reacting a compound of formula (VIII) with acetaldehyde to produce a compound of formula (IX), ii) deesterifying the carboxy protecting group of the compound of formula (IX) using an acid to yield a compound of formula (X), iii) converting the compound of formula (X) to a compound of formula (XI), iv) neutralizing the compound of formula (XI) followed by enzymatic hydrolysis to produce an APCA of formula (V), v) silylating the APCA using a mixture of trimethylsilylchloride and hexamethyldisilazane to produce silylated APCA of formula (XII), and vi) condensing the silylated APCA with a mixed anhydride to produce the DMF solvate compound of formula (I).
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