CAS: 501357-89-7; 8-Chloro[1,2,4]Triazolo[4,3-A]Pyridine

相似化合物

1048913-70-7 929000-42-0 1505568-26-2

上下游产品

formic acid (3-chloro-2-pyridyl)hydrazine 4-ethoxy-1,1,1-trifluoro-3-butene-2-one formaldehyd

📜2,3-二氯吡啶置于hydrazine Hydrate,咪唑盐酸盐体系中,用 乙醇 作为反应溶剂,化学反应生成 8-氯-[1,2,4]三唑并[4,3-A]砒啶
参考文献:使用dmf及其衍生物作为单碳源的无金属[4 + 1]和[5 + 1]环化反应制备杂环
标题:使用dmf及其衍生物作为单碳源的无金属[4 + 1]和[5 + 1]环化反应制备杂环
摘要:1,2,4-三唑并[3,4-A]吡啶和相关的杂环以及取代的三嗪是在各种药物和农用化学试剂中普遍发现的支架.在这里,我们报告了一种高效且实用的方法,该方法使用dmf及其衍生物进行[4 + 1]和[5 + 1]环化反应,以制备这些杂环.这种无金属的反应利用了贮存稳定的dmf作作为反应溶剂和碳供体,使用咪唑氯化物作为催化剂的优势,温和的反应条件可耐受广泛的底物范围并替代.制备的3-未取代的1,2,4-三唑并[3,4-A]吡啶和衍生物允许在3-位进一步引入各种官能团.
DOI:10.1016/j.Tetlet.2020.151844

专利信息

专利号:US-2024239799-A1
优先权日:2021-04-02
标 题:(s)-1-(5-((pyridin-3-yl)thio)pyrazin-2-yl)-4'h,6'h-spiro[piperidine-4,5'-pyrrolo [1,2-b]pyrazol]-4'-amine derivatives and similar compounds as shp2 inhibitors for the treatment of e.g. cancer
发明人：DI FABIO ROMANO; MONTALBETTI CHRISTIAN; PETROCCHI ALESSIA; GRILLO ALESSANDRO; RANDAZZO PIETRO; ROSSETTI ILARIA; CIAMMAICHELLA ALINA
权利人:C N C C S S C A R L COLLEZIONE NAZ DEI COMPOSTI CHIMICI E CENTRO SCREENING; IRBM S P A
摘要:The present invention relates to compounds of formula (I). The compounds of the formula (I) are e.g. (S)-1-(5-((pyridin-3-yl)thio) pyrazin-2-yl)-41H,6′H-spiro[piperidine-4,5′-pyrrolo[1,2-b]pyrazol]-41-amine derivatives and similar compounds. The present invention also relates to the compounds of formula (I) for use as Src homology phosphotyrosine phosphatase 2 (SHP2) inhibitors in methods of treatment of e.g. cancer, cardiovascular diseases, immunological disorders, autoimmune disorders, fibrosis, ocular disorders, systemic lupus erythematosus, diabetes, neutropenia, and combinations thereof. The present invention also relates to pharmaceutical compositions containing said compounds and to their methods of synthesis.