Dinoprost → Prostaglandin E2

Participants

Reaction Steps

The scheme (A) indicates that a regioselectively silylated compound, i.e., bis-triethylsilyl-PGF2α, triethylsilyl ester, can be obtained by reacting PGF2α, with TESiD under 15˜35° C. for 18˜36 hours. Next, the oxidation of the 9-hydroxy group into ketone group is carried out by reacting with a Cr (VI)-based reagent under 15˜35° C. for 10˜15 minutes or activated dimethyl sulfoxide reagent under −78° C. for 2˜3 hours. Last, PGE2 is obtained via a desilylation reaction performed in an acidic aqueous solution reagent having pH=4˜6 under 15˜35° C. for 12˜24 hours.

Provenance & Evidence