发明名称 |
PROCESS FOR PENEMS |
摘要 |
<p>There is provided a process for the preparation of compounds of formula (I) useful as antibacterials, wherein R represents hydrogen atom or a hydroxy protecting group, which process comprises reacting a compound of formula (II) wherein R is as defined above, with an oxalyl halide in an inert solvent; optionally converting the resultant compound of formula (III) wherein R is as defined above and X is a halogen atom into a compound of formula (III) in which X represents a hydroxy group by hydrolysis; either (i) treating the compound of formula (III) in which X is a halogen atom with a compound of formula (IV) wherein Y is a hydroxy group in the presence of an acid scavenger or an organic or inorganic base or (ii) treating the compound of formula (III) in which X is a hydroxy group, with a compound of formula (IV) in which Y is a leaving group in the presence of a base; cyclizing the resultant compound of the formula (V) wherein R is as defined above and optionally deprotecting the resultant compound of formula (I) wherein R is a hydroxy protecting group to obtain a compound of formula (I) wherein R is a hydrogen atom.</p> |
申请公布号 |
WO9100283(A1) |
申请公布日期 |
1991.01.10 |
申请号 |
WO1990EP01060 |
申请日期 |
1990.07.03 |
申请人 |
FARMITALIA CARLO ERBA S.R.L. |
发明人 |
PERRONE, ETTORE;ALPEGIANI, MARCO;ZARINI, FRANCO;MAZZINI, GIUSEPPE;FRANCESCHI, GIOVANNI |
分类号 |
A61K31/43;A61K31/431;A61P31/04;C07D;C07D317/40;C07D499/06;C07D499/88;C07D499/883;C07D499/897 |
主分类号 |
A61K31/43 |
代理机构 |
|
代理人 |
|
主权项 |
|
地址 |
|