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    • 8. 发明申请
    • PROLINE CCI-779 (PROLINE-RAPAMYCIN 42-ESTER WITH 2,2-BIS (HYDROXYMETHYL) PROPIONIC ACID) AND TWO-STEP ENZYMATIC SYNTHESIS OF PROLINE CCI-779 AND CCI-779 USING MICROBIAL LIPASE
    • PROLINE CCI-779(具有2,2-BIS(羟基甲基)丙酸的PROLINE-RAPAMYCIN 42-ESTER)和使用微生物脂蛋白的丙烯酸CCI-779和CCI-779的两步酶合成
    • WO2005100366A1
    • 2005-10-27
    • PCT/US2005/012030
    • 2005-04-12
    • WYETHGU, JianxinRUPPEN, Mark, E.RAVEENDRANATH, PanolilCHEW, WarrenSHAW, Chia-Cheng
    • GU, JianxinRUPPEN, Mark, E.RAVEENDRANATH, PanolilCHEW, WarrenSHAW, Chia-Cheng
    • C07D498/18
    • C07D498/08
    • Disclosed are proline-rapamycin 42-ester with 2,2-bis(hydroxymethyl)propionic acid (proline-CCI-779) as well as a method for the regiospecific preparation of a rapamycin 42-ester or proline-rapamycin 42-ester with 2,2-bis(hydroxymethyl)propionic acid (CCI-779 and proline-CCI-779) comprising the steps of: (a) reacting rapamycin or proline-rapamycin with an activated ester derivative of 2,2-bis(hydroxymethyl)propionic acid having the structure (A) wherein R 1 and R 2 are hydrogen, or taken together to form a ketal with the structure (B) wherein R 3 and R 4 are each, independently, hydrogen, C 1-6 alkyl, either linear or branched, or taken together form C 5-7 cycloalkyl or taken together form cyclic boronate with the structure (C), wherein R 5 is selected from methyl, ethyl, n-propyl, iso-propyl, n-butyl, iso-butyl and phenyl; in a suitable organic solvent in the presence of an effective amount of microbial lipase; and (b) deprotecting the intermediate resulting from step (a) to provide CCI-779 or proline-CCI-779.
    • 公开的是具有2,2-双(羟甲基)丙酸(脯氨酸-CII-779)的脯氨酸 - 雷帕霉素42-酯以及用于区域特异性制备雷帕霉素42-酯或脯氨酸 - 雷帕霉素42-酯的方法,其具有2 包括以下步骤:(a)将雷帕霉素或脯氨酸 - 雷帕霉素与2,2-双(羟甲基)丙酸的活化酯衍生物反应,得到2-双(羟甲基)丙酸(CCI-779和脯氨酸-CII-779) 具有结构(A),其中R 1和R 2是氢,或者一起形成具有结构(B)的缩酮,其中R 3和R 4各自独立地是氢,直链或支链的C 1-6烷基或一起 形成C 5-7环烷​​基或一起形成具有结构(C)的环状硼酸酯,其中R 5选自甲基,乙基,正丙基,异丙基,正丁基,异丁基和苯基; 在合适的有机溶剂中,在有效量的微生物脂肪酶存在下, 和(b)将步骤(a)得到的中间体脱保护,得到CCI-779或脯氨酸-CII-779。