Abstract
In order to prepare ampicillin prodrugs conveniently for practical use, a new synthetic method for 6β-aminopenicillanic acid (6-APA) esters as key intermediates of various ampicillin prodrugs has been developed. Acylation of 6-APA esters to ampicillin esters was achieved in good yields by using phenylglycyl chloride hydrochloride in dichloromethane in the presence of sodium bicarbonate and amide, or ammonium bicarbonate alone. KBT-1585, bacampicillin, talampicillin and pivampicillin have been obtained in good yields by this procedure.
Original language | English |
---|---|
Pages (from-to) | 4316-4322 |
Number of pages | 7 |
Journal | Chemical and Pharmaceutical Bulletin |
Volume | 32 |
Issue number | 11 |
DOIs | |
Publication status | Published - 1984 |
Externally published | Yes |
All Science Journal Classification (ASJC) codes
- Chemistry(all)
- Drug Discovery