主权项 |
1. A method of preparing a chiral sulfone having formula I as a statin intermediate, comprising: (a) reducing a dioxo compound having formula II with a reducing agent to form a dihydroxy compound of formula II-1; (b) protecting the hydroxy groups of the dihydroxy compound of formula II-1 to form a 1,3-dioxane compound of formula II-2; and (c) oxidizing the 1,3-dioxane compound of formula II-2 with an oxidizing agent to form the chiral sulfone, wherein R1 is aryl or heterocyclyl, where the aryl or heterocyclyl is optionally unsubstituted or substituted with one or more substituents, where each of the substituents is independently alkyl, aryl, arylalkyl, halo, cycloalkyl, trifluoromethyl, nitro, cyano, trifluoromethoxy, amido, alkylcarbonyl, thiol or alkylthio; each of R11 and R12 is independently alkyl; and R2 is alkyl, cycloalkyl, arylalkyl, heterocyclyl, aryl or benzyloxycarbonyl. |