摘要
雌笛A环的羟甲基化和咪唑甲基化是两类重要反应,能增大雌甾的亲水性能,改变雌甾的化学性质和生理活性。在进行甾体仿酶模型的设计合成时。
Direct bis-hydroxymethylation and bis-imidazolylmethylation of steroidal estrogenswere studied. Estradiol, 17 α-ethynylestradiol. estroneor estrone 17-ethylene ketal was treatedwith paraformaldehyde respectively, at 50~55℃ in dioxane in the presence of solid sodiumhydroxide to give the corresponding 2, 4-bis(hydroxymethyl)estrogens. Estrogens were treatedwith paraformaldehyde and imidazole at 130~140℃, or via bis-hydroxymethylation thenwith imidazole to give the corresponding 2, 4-bis(imidazolylmethyl) estrogens.
出处
《有机化学》
SCIE
CAS
CSCD
北大核心
1992年第4期396-399,共4页
Chinese Journal of Organic Chemistry
基金
国家自然科学基金
关键词
雌甾
双羟甲基化
双咪唑甲基化
estrogen
bis-hydroxymethylation
bis-imidazolylmethylation
2, 4-bis(hydroxymethyl) estrogen
2, 4-bis(imidazolylmethyl) estrogen