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1. 发明授权

US06803463B2 Process for the preparation of pyrazolopyridine derivatives 失效
标题翻译：吡唑并吡啶衍生物的制备方法
公开(公告)号：US06803463B2
公开(公告)日：2004-10-12
申请号：US10168002
申请日：2002-06-14
申请人： Neil Mathews , Richard Anthony Ward , Andrew Jonathan Whitehead
发明人： Neil Mathews , Richard Anthony Ward , Andrew Jonathan Whitehead
IPC分类号： C07D48704
CPC分类号： C07D487/04 , C07C317/24 , C07D237/08
摘要： A process for the preparation of a compound of formula (I) and pharmaceutically acceptable derivatives thereof in which: R0 is halogen, C1-6alkyl, C1-6alkoxy, C1-6alkoxy substituted by one or more fluorine atoms, or O(CH2)nNR4R5; R1 and R2 are independently selected from H, C1-6alkyl, C1-6alkyl substituted by one or more fluorine atoms, C1-6alkoxy, C1-6hydroxyalkyl, SC1-6alkyl, C(O)H, C(O)C1-6alkyl, C1-6alkylsulphonyl, C1-6alkoxy substituted by one or more fluorine atoms, O(CH2)nCO2C1-6alkyl, O(CH2)nSC1-6alkyl, (CH2)nNR4R5, (CH2)nSC1-6alkyl or C(O)NR4R5; with the proviso that when R0 is at the 4-position and is halogen, at least one of R1 and R2 is C1-6alkylsulphonyl, C1-6alkoxy substituted by one or more fluorine atoms, O(CH2)nCO2C1-6alkyl, O(CH2)nSC1-6alkyl, (CH2)nNR4R5 or (CH2)nSC1-6alkyl, C(O)NR4R5; R3 is C1-6alkyl or NH2; R4 and R5 are independently selected from H, or C1-6alkyl or, together with the nitrogen atom to which they are attached, form a 4-8 membered saturated ring; and n is 1-4.
摘要翻译：一种制备式（I）化合物及其药学上可接受的衍生物的方法，其中：R 0是卤素，C 1-6烷基，C 1-6烷氧基，被一个或多个氟原子取代的C 1-6烷氧基或O（ CH 2）n NR 4 R 5; R 1和R 2独立地选自H，C 1-6烷基，被一个或多个氟原子取代的C 1-6烷基，C 1-6烷氧基，C 1-6羟烷基，SC 1 C（O）H，C（O）C 1-6烷基，C 1-6烷基磺酰基，被一个或多个氟原子取代的C 1-6烷氧基，O（CH 2）n CO 2 C 1-6烷基，O（CH 2）nSC 1-6烷基，）nNR 4 R 5，（CH 2）nSC 1-6烷基或C（O）NR 4 R 5; 条件是当R 0在4-位且是卤素时，R 1和R 2中的至少一个是C 1-6烷基磺酰基，被一个或多个氟原子取代的C 1-6烷氧基，O（ O（CH 2）n C 1-6烷基，（CH 2）n NR 4 R 5或（CH 2）nSC 1-6烷基，C（O）NR 4 R 5; R 3，是C 1-6烷基或NH 2; R 4和R 5独立地选自H或C 1-6烷基，或与它们所连接的氮原子一起形成4-8元饱和环; 而且是1-4。

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