CAS: 428854-24-4; 2-(1-(2-Fluorobenzyl)-1H-Pyrazolo[3,4-B]Pyridin-3-yl)Pyrimidine-4,5,6-Triamine

相似化合物

1350653-30-3 1702271-98-4 1169770-52-8

上下游产品

2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-5-[(E)-phenyldiazen-1-yl]pyrimidine-4,6-diamine (2-fluorobenzyl)hydrazine 1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridine-3-carbonitrile ethyl 5-amino-1-(2-fluorobenzyl)-1H-pyrazole-3-carboxylate N'-[2-(tert-butyl-dimethyl-silanyloxy)-ethyl]-2-[1-(2-fluoro-benzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-pyrimidine-4,5,6-triamineN'-[2-(tert-butyl-dimethyl-silanyloxy)-ethyl]-2-[1-(2-fluoro-benzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-pyrimidine-4,5,6-triamine Ri°Ciguat 6-amino-7-(2-{[tert-butyl(dimethyl)silyl]oxy}ethyl)-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-7,9-dihydro-8H-purin-8-one 6-amino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-7-(2-hydroxyethyl)-7,9-dihydro-8H-purin-8-one

1-(2-氟苄基)-1H-吡唑并[3,4-B]吡啶-3-甲腈置于镍 氢气,Sodium Methylate,氯化铵,溶剂黄146体系中,用 甲醇,N,N-二甲基甲酰胺 作为反应溶剂,20.0~110.0 °C,6.5 Mpa 条件下,反应 44.0H,反应生成 2-[1-(2-氟苄基)-1H-吡唑并[3,4-B]吡啶-3-基]嘧啶-4,5,6-三胺
参考文献:Metabolites Of Orally Active No-Independent Pyrazolopyridine Stimulators Of Soluble Guanylate Cyclase
标题:Metabolites Of Orally Active No-Independent Pyrazolopyridine Stimulators Of Soluble Guanylate Cyclase
摘要:The Pyrazolopyridine Stimulators Of Soluble Guanylate Cyclase Bay 41-2272 And 41-8543 Were Oxidised In Rats And Dogs At Their 5-Pyrimidinyl-Cyclopropyl And-Morpholino Residue. These Metabolites Activate The Soluble Guanylate Cyclase,Induce Vaso-Elaxation And Thereby May Contribute To The In Vivo Activity Of Bay 41-2272 And Bay 41-8543. (C) 2002 Elsevier Science Ltd. All Rights Reserved.
DOI:10.1016/s0968-0896(02)00034-2

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.

专利号:CN-117229282-A
优先权日:2023-09-11
标 题:A kind of synthesis technology of riociguat