摘要
以雌酚酮为起始原料,经硼氢化钠还原制得17β-雌二醇,再经乙酸酐酰化保护羟基和三氧化铬氧化得到3,17-二乙酰基-6-酮-17β-雌二醇,最后经氢氧化钾水溶液水解合成了雌激素药物中间体6-酮雌二醇,总收率38.0%,其结构经1H NMR确证。
3,17-diacetyl-6-oxo-17β-estradiol(5) was prepared from commercially available estrone followed by reduction with NaBH4,acylation with acetic anhydride for protecting hydroxyl and oxidation with CrO3.Then 5 was hydrolyzed by KOH to give an important intermediate of estrogen drug,6-oxo-estradiol in total yield of 38.0%.The structure was confirmed by 1H NMR.
出处
《合成化学》
CAS
CSCD
北大核心
2011年第3期428-429,432,共3页
Chinese Journal of Synthetic Chemistry
基金
国家自然科学基金资助项目(30770655
30472081
81072531)