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    • 10. 发明授权
    • Alternative synthesis of renin inhibitors and intermediates thereof
    • 肾素抑制剂及其中间体的替代合成
    • US08143416B2
    • 2012-03-27
    • US13022243
    • 2011-02-07
    • Gottfried SedelmeierStuart John MickelHeinrich Rueeger
    • Gottfried SedelmeierStuart John MickelHeinrich Rueeger
    • C07D263/52
    • C07D207/26C07C271/16C07C271/22C07D211/76C07D307/33
    • The present invention relates to synthetic routes to prepare a compound of the formula wherein R1 is halogen, C1-6halogenalkyl, C1-6alkoxy-C1-6alkyloxy or C1-6alkoxy-C1-6alkyl; R2 is halogen, C1-4alkyl or C1-4alkoxy; R3 and R4 are independently branched C3-6alkyl; and R5 is cycloalkyl, C1-6alkyl, C1-6hydroxyalkyl, C1-6alkoxy-C1-6alkyl, C1-6alkanoyloxy-C1-6alkyl, C1-6aminoalkyl, C1-6alkylamino-C1-6alkyl, C1-6dialkylamino-C1-6alkyl, C1-6alkanoylamino-C1-6alkyl, HO(O)C—C1-6alkyl, C1-6alkyl-O—(O)C—C1-6alkyl, H2N—C(O)—C1-6alkyl, C1-6alkyl-HN—C(O)—C1-6alkyl or (C1-6alkyl)2N—C(O)—C1-6alkyl; or a pharmaceutically acceptable salt thereof as well as key intermediates obtained when following these routes as well as their preparation.
    • 本发明涉及制备下式化合物的合成路线:其中R 1是卤素,C 1-6卤代烷基,C 1-6烷氧基-C 1-6烷氧基或C 1-6烷氧基-C 1-6烷基; R2是卤素,C1-4烷基或C1-4烷氧基; R3和R4独立地是支链的C 3-6烷基; 和R 5是环烷基,C 1-6烷基,C 1-6羟基烷基,C 1-6烷氧基-C 1-6烷基,C 1-6烷酰氧基-C 1-6烷基,C 1-6氨基烷基,C 1-6烷基氨基-C 1-6烷基,C 1-6二烷基氨基-C 1-6烷基,C 1 (O)C 1-6烷基,C 1-6烷基-O-(O)C 1-6烷基,H 2 N-C(O)-C 1-6烷基,C 1-6烷基-NH- C (O)-C 1-6烷基或(C 1-6烷基)2 N -C(O)-C 1-6烷基; 或其药学上可接受的盐以及按照这些途径获得的关键中间体及其制备方法。