| Transition-metal-catalyzed cross-coupling have achieved giantic progress and been widely applied in organic synthesis. But in this area there are still many challenging task to be solved, catalytic asymmetric coupling of research is one of them. The transition-metal-catalyzed asymmetric coupling reaction research mainly focused on the aryl C-C coupling. In recent years, through palladium catalytic asymmetric as Buchwald-Hartwig coupling to build C-N axis chiral and chiral center have been reported. But for asymmetric aryl C-O coupling reaction, whether to build axis chiral and chiral center are very scarce. Based on the previous research, we developed coupling reaction of asymmetric desymmetric to build C-O bond. The main content of this paper focuses on: through Pdlladium-catalyzed asymmetric desymmetric coupling reaction for building the chiral o-Heterocycles. Basing on these, simple synthetic drug molecules with the same skeleton. Fully reflects the asymmetic C-O coupling reaction is practical. Part ⅠPd-Catalyzed Asymmetric C-O Coupling ReactionStarting from 2-(2-iodophenoxy)propane-1,3-diol, under the Pd(OAc)2 and SDP(O) ligand, we synthesied the(S)-(2,3-dihydrobenzo[b] [1,4]dioxin-2-yl)methanols in highly enantioselectively through intramolecular C-O coupling. The product enantiomeric excesse could up to 97%, yiled 98%. PartⅡ Asymmetric C-O coupling reaction in the application of the drug molecules synthesisIn the partⅠof asymmetric C-O coupling reaction products as raw materials, to simpel synthetic drug molecules such as MKC-242, WB4101. Shorten the synthetic route of this kind of drug molecules, reduce the cost of synthesis, to reduce pollution and protect the environment.In this paper, by means of asymmetric desymmetric, studied PdCatalyzed Asymmetric C-O Coupling Reaction in detail. Successful formation of the C-O bond with chiral center. At the same time, it is significant advantages to synthesized the chiral drug molecules. |
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