PROCESS FOR PREPARING ALPHA-AMINO-P-HYDROXY-BENZYL-PENICILLINE-TRIHYDRATE

During an improved prepn. of alpha-amino-p-hydroxy -benzylpenicillin-trihydrate, (-5)-(-10 deg.) C is used for a rapid and stable formation of the mixed anhydride. At the end of the reaction sequence but prior to the splitting off the protective gp. hydrochloric acid is added to the reaction mix at...

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Hauptverfasser: KARACSONYI,NEE KISS,ANIKO,HU, ELEK,SANDOR,HU, NAGY,JOZSEF,HU, ANTAL,ERNOE,HU, KELEN,TIBOR,HU, BORBELY,SZABOLCS,HU, BALINT,MARTA,HU, MELCZER,ISTVAN,HU, KOCSAR,BARNA,HU, NEMES,SANDOR,HU, ZSUGA,MIKLOS,HU
Format: Patent
Sprache:eng
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Zusammenfassung:During an improved prepn. of alpha-amino-p-hydroxy -benzylpenicillin-trihydrate, (-5)-(-10 deg.) C is used for a rapid and stable formation of the mixed anhydride. At the end of the reaction sequence but prior to the splitting off the protective gp. hydrochloric acid is added to the reaction mix at (-55)-(-75) deg. C to avoid an acidity excess. Following the mixing stage, the temp. is raised to 0 deg. C, the optimum temp. for hydrolysis. Using above method the product is obtd. at 80% yield and is of pharmacopoeial quality.