Estradiol 3-N-bis(2-chloroethyl)carbamate (IV) was prepared by treatment of estradiol (I) with either the carbamoyl chloride (II) or the carbamoyl bromide (III) in the presence of various bases such as triethylamine and DMAP or DBU. Phosphorylation of (IV) with phosphorus oxychloride and pyridine, followed by aqueous hydrolysis, produced the 17-O-phosphate ester (V). This was converted to the corresponding disodium salt by treatment with sodium methoxide.

Estradiol 3-N-bis(2-chloroethyl)carbamate (IV) was prepared by treatment of estradiol (I) with either the carbamoyl chloride (II) or the carbamoyl bromide (III) in the presence of various bases such as triethylamine and DMAP or DBU. Phosphorylation of (IV) with phosphorus oxychloride and pyridine, followed by aqueous hydrolysis, produced the 17-O-phosphate ester (V). This was converted to the corresponding disodium salt by treatment with sodium methoxide.

Estradiol 3-N-bis(2-chloroethyl)carbamate (IV) was prepared by treatment of estradiol (I) with either the carbamoyl chloride (II) or the carbamoyl bromide (III) in the presence of various bases such as triethylamine and DMAP or DBU. Phosphorylation of (IV) with phosphorus oxychloride and pyridine, followed by aqueous hydrolysis, produced the 17-O-phosphate ester (V). This was converted to the corresponding disodium salt by treatment with sodium methoxide.