专利号:US-8957210-B2 优先权日:2011-12-12 标题:Method for synthesizing 1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridine-3-formamidine hydrochloride 发明人:LI JIN; YANG XIAOYU; ZHU JINGWEI; YANG MINMIN; WU XIHAN 权利人:PHARMABLOCK NANJING R & D CO LTD 摘要:The present invention relates to the field of chemical synthesis, and in particular to a method for synthesizing 1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-formamidine hydrochloride, which is an important intermediate of Riociguat that is an anti-thromboembolic-disease medicine. The method is characterized in that: 3-iodo-1H-pyrazolo[3,4-b]pyridine is used as a raw material; the raw material is reacted with fluorobenzyl bromide to form a compound (10); the compound (10) is reacted with zinc cyanide to form a compound (6); the compound (6) is reacted with sodium methoxide, ammonium chloride, acetic acid and methanol to form a compound (8); and the compound (8) is reacted with chlorine hydride gas to form 1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-formamidine hydrochloride. The method has the characteristics of cheap and readily available raw materials, high yield, mild reaction conditions and the like, and is a synthesis method having a large-scale preparation value.
专利号:US-7541367-B2 优先权日:2005-05-31 标 题 :3-benzoimidazolyl-pyrazolopyridines useful in treating kinase disorders 发明人:CHIU GEORGE; CONNOLLY PETER J; EMANUEL STUART; HUANG SHENLIN; LI SHENGJIAN; LIN RONGHUI; LU YANHUA; MIDDLETON STEVEN A 权利人:JANSSEN PHARMACEUTICA NV 摘要:The present invention is directed to novel 3-benzoimidazolyl-pyrazolopyridine compounds of formula (I): n nand pharmaceutically acceptable forms thereof and their synthesis and use as inhibitors of serine-threonine protein kinases and tyrosine protein kinases and interactions thereof.
参考文献:10.1055/s-0037-1610783 摘要:Keating JJ, Alam RM. An Expedient Approach to Pyrazolo[3,4-b]pyridine-3-carboxamides via Palladium-Catalyzed Aminocarbonylation. Synthesis. 2021 Aug 26;53(24):4709–22. doi: 10.1055/s-0037-1610783.