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    • 7. 发明公开
    • CEPHALOMANNINE EPOXIDE, ITS ANALOGUES AND A METHOD FOR PREPARING THE SAME
    • CEPHALOMANNIN-EPOXID,DESSEN ANALOGON UND EIN VERFAHREN ZU DESSEN HERSTELLUNG
    • EP0815096A4
    • 1998-07-08
    • EP96909628
    • 1996-03-08
    • HAUSER CHEMICAL RES INC
    • ZHENG QUN YMURRAY CHRISTOPHER KDAUGHENBAUGH RANDALL J
    • A61K31/335A61K31/337A61P35/00C07D305/14C07D407/12
    • C07D407/12C07D305/14
    • An antitumor compound of formula (5), in which R = Ac or H, and R1 = R2 = an alkyl group such as Me, Et, Pr, i-Pr, n-Bu or t-Bu, R3 = H; R1 = R2 = R3 = H; R1 = an alkyl group such as Me, Et, Pr, i-Pr, n-Bu or t-Bu, R2 = R3 = H; R1 = R3 = H, R2 = an alkyl group such as Me, Et, Pr, i-Pr, n-Bu or t-Bu; R1 = H, R2 = R3 = an alkyl group such as Me, Et, Pr, i-Pr, n-Bu or t-Bu; R1 = R2 = R3 = an alkyl group Me, Et, Pr, i-Pr, n-Bu or t-Bu. Me is an abbreviation for methyl, Et is ethyl, Pr is propyl, i-Pr is isopropyl, n-Bu is n-butyl, and t-Bu is tert-butyl. Also provided by the invention is a one-step method of preparing a compound of formula (5) whereby a taxane having a tiglate group attached to the side chain is contacted with an oxidizing reagent resulting in the formation of an epoxide having antitumor activity.
    • (5)的抗肿瘤化合物,其中R = Ac或H,并且R1 = R2 =烷基如Me,Et,Pr,i-Pr,n-Bu或t-Bu,R3 = H; R1 = R2 = R3 = H; R1 =烷基如Me,Et,Pr,i-Pr,n-Bu或t-Bu,R2 = R3 = H; R1 = R3 = H,R2 =烷基如Me,Et,Pr,i-Pr,n-Bu或t-Bu; R 1 = H,R 2 = R 3 =烷基如Me,Et,Pr,i-Pr,n-Bu或t-Bu; R1 = R2 = R3 =烷基Me,Et,Pr,i-Pr,n-Bu或t-Bu。 Me是甲基的缩写,Et是乙基,Pr是丙基,i-Pr是异丙基,n-Bu是正丁基,并且t-Bu是叔丁基。 本发明还提供了制备式(5)化合物的一步法,其中将具有连接至侧链的惕酸酯基的紫杉烷与氧化剂接触,导致形成具有抗肿瘤活性的环氧化物。