Process for preparing enamine derivatives, compounds so produced and process for preparing a 3-hydroxy-cephalosporin
申请人:Lilly Industries Limited
公开号:EP0019401A1
公开(公告)日:1980-11-26
There is described a process for preparing an enamine of formula (IX):
where R2 is a carboxylic acid protecting group and R3 is the residue of a carboxylic acid derived acyl group and where R5 and R6 are the same or different C1-4 alkyl or C7-10 aralkyl groups; or taken together with the adjacent nitrogen atom form a heterocyclic ring containing from 4 to 8 carbon atoms and optionally a further heteroatom selected from oxygen and nitrogen; by reacting a compound of formula (XII) :
with an amine of formula HNR5R6, the reactant of formula (XII) being prepared by reaction of an appropriate enol derivative with a phosphorus reagent. The enamines of formula (IX) are useful in the preparation of 3-hydroxycephalosporins.
本发明描述了一种制备式(IX)烯胺的工艺:
其中 R2 是羧酸保护基,R3 是羧酸衍生酰基的残基,R5 和 R6 是相同或不同的 C1-4 烷基或 C7-10 芳烷基;或与相邻的氮原子一起形成含有 4 至 8 个碳原子和任选地另一个选自氧和氮的杂原子的杂环;通过使式 (XII) :
与式 HNR5R6 的胺反应,式 (XII) 的反应物通过适当的烯醇衍生物与磷试剂反应制备。式(IX)的烯胺可用于制备 3-羟基头孢菌素。