Imura A, Itoh M, Miyadera A
Chemical Technology Research Laboratories, Daiichi Pharmaceutical Co., Ltd., Tokyo, Japan.
Chem Pharm Bull (Tokyo). 1998 Dec;46(12):1878-80. doi: 10.1248/cpb.46.1878.
The key intermediate of a 20(S)-camptothecin 1 synthesis was obtained in a highly enantioselective fashion using an enzyme-catalyzed resolution. A commercially available protease was found to exhibit the highest enantioselectivity with moderate activity, and (S)-ethyl 2-acetoxy-2-[6-(acetoxymethyl)-1,1-(ethylenedioxy)-5-oxo- 1,2,3,5-tetrahydroindolizin-7-yl]butanoate 7c of 98% e.e. was obtained as the remaining substrate.
通过酶催化拆分以高对映选择性方式获得了20(S)-喜树碱1合成的关键中间体。发现一种市售蛋白酶表现出最高的对映选择性和适度的活性，并以98%的对映体过量获得了(S)-2-乙酰氧基-2-[6-(乙酰氧基甲基)-1,1-(乙二氧基)-5-氧代-1,2,3,5-四氢中氮茚-7-基]丁酸乙酯7c作为剩余底物。
