合成路线1

In an alternative method, the hydroxyl group of estrone (V) was protected as the benzyl ether (VI), which was subsequently subjected to electrophilic nitration to yield selectively the 2-nitro derivative (VII). After reduction of (VII) to the corresponding amine (VIII), replacement of the amino for a methoxy group was performed by diazotization, followed by treatment with sodium methoxide, using Sandmeyer conditions. Finally hydrogenolysis of the O-benzyl protecting group, with simultaneous ketone reduction led to the desired 2-methoxy estradiol.