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    • 6. 发明申请
    • Processes for preparing 4'-azido-nucleoside derivatives
    • 制备4'-叠氮基 - 核苷衍生物的方法
    • US20050038240A1
    • 2005-02-17
    • US10871917
    • 2004-06-18
    • Terrence ConnollyKieran DurkinKeshab SarmaJiang Zhu
    • Terrence ConnollyKieran DurkinKeshab SarmaJiang Zhu
    • C07H19/067C07D45/04
    • C07H19/067
    • A process for the preparation of a 4′-azido-2′,3′,5′-triacyl-nucleoside compound (I; B=B1; R1 is R1aCO— and R2 is R2aCO—) or a 4′-azidonucleoside compounds (I; B is B1 or B2 and R1 and R2 are hydrogen and acid addition salts thereof) wherein R1a and R2a are independently C1-10 alkyl or phenyl optionally substituted with 1 to 3 substituents selected from the group consisting of alkyl, alkoxy, halogen, nitro or cyano and R3 is selected from the group consisting of hydrogen, C1-6 alkyl, C1-3 haloalkyl and halogen, comprising contacting a 5′-iodo compound II with a peracid, R2aC(O)OOH, an acid R2aC(O)OH and a phase transfer catalyst and interconverting a uridine B1 to a cytosine B2. The present process provides the 4′-azidonucleosides safely and selectively in high purity with increased efficiency.
    • 制备4'-叠氮基-2',3',5'-三酰基 - 核苷化合物(I; B = B1; R 1)的方法是R 1aCO-和R 2是R 其中R 1a和R 2a均为氢或其酸加成盐,其中R 1a和R 2a均为 独立地为C 1-10烷基或任选被1至3个选自烷基,烷氧基,卤素,硝基或氰基的取代基取代的苯基,R 3选自氢,C 1-6烷基, 3卤代烷基和卤素,包括使5'-碘化合物II与过酸,R 2a C(O)OOH,酸R 2a C(O)OH和相转移催化剂接触并将尿苷B1互变为 胞嘧啶B2。 本发明方法提供高纯度安全和选择性的4'-叠氮核苷提高效率。