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    • 3. 发明申请
    • METHOD FOR PREPARING ADENINE COMPOUND
    • 制备腺嘌呤化合物的方法
    • US20110054168A1
    • 2011-03-03
    • US12863297
    • 2009-01-16
    • Ayumu KurimotoWataru KatodaKazuki HashimotoKazuhiko Takashi
    • Ayumu KurimotoWataru KatodaKazuki HashimotoKazuhiko Takashi
    • C07D473/18
    • C07D473/18
    • A method for preparing compound (4): wherein m and n are independently an integer of 2 to 5, R1 is C1-6 alkyl group, R2 and R3 are combined with an adjacent nitrogen atom to form pyrrolidine, morpholine, thiomorpholine, etc., and R4 is C1-3 alkyl group, or a pharmaceutically acceptable salt, which is useful as a medicament, which comprises step (a) for preparing compound (2): wherein m, n, R1, R2 and R3 are the same as defined above, or its salt which comprises subjecting compound (1): wherein k is an integer of 1 or 2, R is hydrogen atom, halogen atom, etc., or a salt thereof to debenzylation reaction, and then step (b) for preparing compound (4) or a pharmaceutically acceptable salt which comprises reacting compound (2) or its salt prepared in the above step (a) or salt thereof and compound (3): wherein R4 is C1-3 alkyl group, in the presence of a boron-containing reducing agent.
    • 一种制备化合物(4)的方法:其中m和n独立地为2至5的整数,R 1为C 1-6烷基,R 2和R 3与相邻的氮原子结合形成吡咯烷,吗啉,硫代吗啉等。 ,和R4为C1-3烷基,或其药学上可接受的盐,其可用作药物,其包含用于制备化合物(2)的步骤(a):其中m,n,R 1,R 2和R 3相同 或其盐,其包括使化合物(1):其中k为1或2的整数,R为氢原子,卤素原子等或其盐进行脱苄基化反应,然后步骤(b)为 制备化合物(4)或其药学上可接受的盐,其包括使上述步骤(a)中制备的化合物(2)或其盐或其盐与化合物(3)反应:其中R 4为C 1-3烷基,在 含硼还原剂。