Chemoenzymatic Synthesis of Biologically Active Natural products via Lipase TL -Mediated Kinetic Resolution as a Key Step and their Structure Activity Relationship

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1)Lipase TL-mediated kinetic resolution of 2-pentanol (C5 unit) and 2-propanol (C3 unit) proceeded in the presence of base at low temperature to give the corresponding optically pure alcohols and acetates in good yields, respectively. The 2-pentanol and its acetate thus obtained were converted both enantiomers of piperazic acid derivatives, which are important segments of hexadepsipeptide GE3. 2)Cytotoxic ent-kaurene diterpenes were isolated from Rabdosia excisa to obtained substrates for Lipase TL-mediated regioselective acetylation of polyhydroxy natural products. 3)Efficient transformation of 7,14-dihydroxy-ent-kaurenes to tetracyclic ent-abietanes under Mitsunobu reaction conditions were developed. The tetracyclyc ent-abietanes have been found to be potent cytotoxic agents. 4)SAR study on ent-kaurenes and tetracyclic ent-abietanes were also examined.