CAS: 51859-98-4; (2-Fluorobenzyl)Hydrazine

欧盟法规

[ECHA物质

邻氟氯苄置于hydrazine Hydrate体系中,用 乙醇 作为反应溶剂,以85 %的收率获得产物2-氟苄基肼
参考文献:Cn115947689
标题:Cn115947689

专利信息

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.