药学研究
藥學研究
약학연구
JOURNAL OF PHARMACEUTICAL RESEARCH
2015年
6期
365-367
,共3页
Δ9(11)坎利酮%依普利酮%合成
Δ9(11)坎利酮%依普利酮%閤成
Δ9(11)감리동%의보리동%합성
Δ9(11)-canrenone%Eplerenone%Synthesis
以Δ9(11)坎利酮为起始原料,与氰化钠反应得到烯胺(化合物4),烯胺水解转化为二酮(化合物3)。然后,在甲醇钠条件下,发生开环消除反应得甲酯(化合物2)。最后,在三氯乙酰胺催化下,或者三氯乙酰胺和磷酸氢二钾的共同催化下,经双氧水氧化反应制得终产物依普利酮。
以Δ9(11)坎利酮為起始原料,與氰化鈉反應得到烯胺(化閤物4),烯胺水解轉化為二酮(化閤物3)。然後,在甲醇鈉條件下,髮生開環消除反應得甲酯(化閤物2)。最後,在三氯乙酰胺催化下,或者三氯乙酰胺和燐痠氫二鉀的共同催化下,經雙氧水氧化反應製得終產物依普利酮。
이Δ9(11)감리동위기시원료,여청화납반응득도희알(화합물4),희알수해전화위이동(화합물3)。연후,재갑순납조건하,발생개배소제반응득갑지(화합물2)。최후,재삼록을선알최화하,혹자삼록을선알화린산경이갑적공동최화하,경쌍양수양화반응제득종산물의보리동。
With Δ9(11)-canrenone as raw material,eplerenone was obtained after a series of reaction process,inclu-ding sodium cyanide addition to give enamine( compound 4),hydrolysis to diketone( compound 3). After ring opening and eliminating in presence of sodium methoxide,diketone(compound 3)was converted to methyl ester(compound 2). Finally, epoxidation of compound 2 was performed by reaction with H2 O2 in the presence of trichloroacetamide or trichloroacetonitrile and K2 HPO4 ,giving eplerenone.