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    • 1. 发明申请
    • INTERMEDIATE COMPOUNDS USEFUL FOR MAKING ANTIVIRAL COMPOUNDS
    • 用于制备抗病毒化合物的中间体化合物
    • WO2002059132A1
    • 2002-08-01
    • PCT/US2002/002338
    • 2002-01-28
    • VIROPHARMA INCORPORATEDRYS, David, J.NITZ, Theodore, J.
    • RYS, David, J.NITZ, Theodore, J.
    • C07F7/02
    • C07F7/1856C07C45/59C07C45/60C07C45/71C07C47/575C07D317/22C07D319/06
    • Novel compounds of Formula I and Formula II (below): formula (I) wherein R a is selected from the group consisting of -CH 2 -OCH 3 , -CH 2 -OCH 2 CH 3 , -CH(CH 3 )OCH 2 CH 3 , -CH 2 -OCH 2 CH 2 -OCH 3 , -CH 2 OCH 2 CH 2 -Si(CH 3 ) 3 , and formula (II); R 1 is a radical selected from the group consisting of hydrogen, halogen, perfluoroalkyl, nitro, carbalkoxy, carboxamide, carboxamidoalkyl, alkyl, cycloalkyl, alkoxy, alkoxyalkyl, alkoxy-C 2 -C 6 -alkoxy, alkylsulfinyl, alkylsulfonyl, sulfonamide, cyano, amido, dialkylamino, OR a , or a heterocyclic radical selected from the group consisting of morpholinyl, piperadinyl, pyrrolidinyl, or an N-substituted piperazinyl, said piperazinyl substituents selected from an alkyl group, the point of attachment of said heterocyclic radical is at a nitrogen atom; P is a protected formaldehyde group such as: formula (III) or formula (IV) wherein R 2 , R 3 , R 4 and R 5 are independently selected from the group consisting of hydrogen or alkyl. The compounds are useful for making antiviral agents.
    • 式I和式II的新型化合物(下文):其中R a选自-CH 2 -OCH 3,-CH 2 -OCH 2 CH 3,-CH(CH 3)OCH 2 CH 3,-CH 2 -OCH 2 CH 2 -OCH 3, - CH 2 OCH 2 CH 2 -Si(CH 3)3和式(II); R 1是选自氢,卤素,全氟烷基,硝基,烷氧基,羧酰胺,甲酰氨基烷基,烷基,环烷基,烷氧基,烷氧基烷基,烷氧基-C 2 -C 6 - 烷氧基,烷基亚磺酰基,烷基磺酰基,磺酰胺,氰基,酰胺基, 二烷基氨基,ORa或选自吗啉基,哌啶基,吡咯烷基或N-取代的哌嗪基的杂环基,所述哌嗪基取代基选自烷基,所述杂环基的连接点在氮原子上; P是受保护的甲醛基团,例如:式(III)或式(IV)其中R2,R3,R4和R5独立地选自氢或烷基。 该化合物可用于制备抗病毒剂。