| 摘要 |
<p>This invention relates to the phthalide ester of 6-D(-).alpha.-aminophenylacetamido! penicillanic acid and its pharmaceutically acceptable acid addition salts, and to a process for its preparation. The esters of the invention are novel and are useful in that they produce high serum concentrations of the parent penicillin when administered orally, and higer than can be achieved with the parent penicillin itself. The esters of the present invention may be prepared by a process which comprises reacting 6-aminopenicillanic acid phthalide ester or a silyl derivative thereof with a reactive Nacylating derivative of the (D) isomer of a compound of the formula: wherein X is an amino group, a protected amino group or a group which is convertible to an amino group, removing the silyl group, if present, by hydrolysis or alcoholysis, and if X is not an amino group, converting it to such a group under neutral or acid conditions. 6-aminopenicillanic acid phthalide ester is a novel compound and its preparation is also disdisclosed as well as salts of this compound.</p> |
