申请人:BEECHAM GROUP PLC
公开号:EP0038661A2
公开(公告)日:1981-10-28
A process for the preparation of a lactam of formula:
wherein R1, R2 and R3 may be the same or different and each represents hydrogen or C1-6 alkyl, or R1 and R2 may together complete a carbocyclic ring; R4 is hydrogen, -CH -CO2RP where RP is a carboxy-protecting group, -CH2-CH2-OH or a protected derivative thereof, -CH2-CH2-CHO or a protected derivative thereof, or R3 and R4 together complete a carbocyclic ring; R4 is hydrogen or C1-6 alkyl; and R5 is hydrogen, an organic radical wherein any reactive groups may be protected or a subgroup offormula-NRαRβ wherein Rα and Rβ are the same or different and each is hydrogen or an organic radical, or a subgroup of ORδ wherein Rδ is a hydroxyl protecting group, which process comprises treatment of an iron complex of formula
with an oxidising agent.
一种制备式内酰胺的工艺:
其中R1、R2和R3可以相同或不同,各自代表氢或C1-6烷基,或R1和R2可共同完成一个碳环;R4是氢、-CH -CO2RP(其中RP是羧基保护基团)、-CH2-CH2-OH或其保护衍生物、-CH2-CH2-CHO或其保护衍生物,或R3和R4共同完成一个碳环;R4 是氢或 C1-6 烷基;以及 R5 是氢、有机基(其中任何活性基团均可被保护)或式-NRαRβ 的子基团(其中 Rα 和 Rβ 相同或不同且各自是氢或有机基)或 ORδ 的子基团(其中 Rδ 是羟基保护基)。
该工艺包括用氧化剂处理式铁络合物。