CAS: 256376-62-2; 1-(2-Fluorobenzyl)-1H-Pyrazolo[3,4-B]Pyridine-3-Carboxamide

该化合物是一种化学化合物,其特点是其基体结构,即双环化合物,具有双环和双甲醇和环,通常具有有机溶剂中溶性以及由于碳箱酰胺功能组的存在而具有潜在生物活动等特性,这些特性可以参与氢结合并影响其与生物目标的相互作用;2氟苯组的存在可能提高其亲性并改变其药用动力特性;该化合物对医药化学具有兴趣,特别是其可能用于药物开发的潜力,因为已探索了-结构的衍生物,以产生各种治疗效应,包括防炎和抗癌活动;其分子结构和功能组表明,它可能与生物巨型分子进行具体互动,从而成为进一步开展药理学和药用化学研究的候选对象.

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256376-65-5 256499-19-1 1350653-27-8

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上下游产品

CAS号256376-59-7 1-(2-fluorobenz... | CAS号51859-98-4 2-氟苄基肼 | CAS号256504-39-9 5-氨基-1-(2-氟苄基)-... | CAS号256376-68-8 1-(2-氟苄基)-1H-吡唑... | CAS号256376-65-5 1-(2-氟苄基)-1H-吡唑... | CAS号256376-24-6 BAY 41-2272

合成工艺路线路线简述

    📜1-(2-氟苄基)-1H-吡唑并[3,4-B]吡啶-3-羧酸乙酯 反应生成1-[(2-氟苯基)甲基]-1H-吡唑并[3,4-B]吡啶-3-羧酰胺
    参考文献:Substituted Pyrazole Derivatives Condensed With Six-Membered Heterocyclic Rings
    标题:Substituted Pyrazole Derivatives Condensed With Six-Membered Heterocyclic Rings
    摘要:本发明涉及一种新型的取代吡唑衍生物,其通式为(i),其中r1,R2,R3和a分别如定义所述,并涉及其制备过程以及作为药物的用途,特别是作为治疗心血管疾病的药物.

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    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.

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    合成参考文献

    参考DOI号:10.1016/S0960-894X(01)00073-7
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