Process for the preparation of 2-halomethyl-penems and their use for the
preparation of antibacterial penems
    12.
    发明授权
    Process for the preparation of 2-halomethyl-penems and their use for the preparation of antibacterial penems 失效
    制备2-卤代甲基青铜的方法及其用于制备抗菌青铜的方法

    公开(公告)号:US6153747A

    公开(公告)日:2000-11-28

    申请号:US130264

    申请日:1998-08-06

    摘要: Process for the preparation of 2-halomethyl-penems (I) comprising (a) reacting an acetoxy-(protected hydroxyethyl)-2-azetidinone (III) with a 2-halothioacetic acid to form a 3-haloacetylthioazetidinone (V), (b) reacting (V) with oxalyl chloride to give an intermediate (VII), acylated on the beta-lactamic nitrogen, and (c) cyclizing (VII) in the presence of an organic phosphate or phosphonite to produce the corresponding 2-halomethyl-penem (I).

    摘要翻译: (I)的制备方法,包括(a)使乙酰氧基 - (被保护的羟乙基)-2-氮杂环丁酮(III)与2-卤代硫代乙酸反应以形成3-卤代乙酰基硫代氮杂环丁酮(V),(b) )使(V)与草酰氯反应得到在β-内酰胺氮上酰化的中间体(VII),和(c)在有机磷酸盐或亚膦酸盐存在下环化(VII)以产生相应的2-卤代甲基 - (一世)。