Objective To synthesize the angiogenesis inhibitor, 2-methoxylestradiol. Methods 2-Methoxylestradiol was obtained by acylation, Frise rearrangement, protection of 3-hydroxyl, hydrolyzation, 2-methylation, and deprotection of 3-benzyl ether. Results Comparing to the reported method, one reaction step was shortened and the overall yield of improved reaction sequence was raised 10%.The structure of obtained 2-methoxyestradiol was confirmed with 1H-NMR and mass spectrum. Conclusions Compared with the reported methods, we improved 6 steps among this 7-steps reaction sequence. The improved procedure is more concise and practical.
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