中国医药工业杂志
中國醫藥工業雜誌
중국의약공업잡지
CHINESE JOURNAL OF PHARMACEUTICALS
2010年
4期
249-250
,共2页
匡仁云%郭瑾%周小春%黄春芳
劻仁雲%郭瑾%週小春%黃春芳
광인운%곽근%주소춘%황춘방
3-碘-1H-吡唑并[3,4-b]吡嗪%中间体%合成
3-碘-1H-吡唑併[3,4-b]吡嗪%中間體%閤成
3-전-1H-필서병[3,4-b]필진%중간체%합성
3-iodo-1H-pyrazolo [3,4-6] pyrizine%intermediate%synthesis
2-氰基吡嗪和氯化亚砜在DMF作用下反应得3-氯-2-氰基吡嗪,经水合肼闭环得3-氨基-1H-吡唑并[3,4-6]吡嗪,再经NaNO_2/p-TsOH/K1一步完成重氮化-碘代反应得到3-碘-1H-吡唑并[3,4-b]吡嗪,总收率约31%.
2-氰基吡嗪和氯化亞砜在DMF作用下反應得3-氯-2-氰基吡嗪,經水閤肼閉環得3-氨基-1H-吡唑併[3,4-6]吡嗪,再經NaNO_2/p-TsOH/K1一步完成重氮化-碘代反應得到3-碘-1H-吡唑併[3,4-b]吡嗪,總收率約31%.
2-청기필진화록화아풍재DMF작용하반응득3-록-2-청기필진,경수합정폐배득3-안기-1H-필서병[3,4-6]필진,재경NaNO_2/p-TsOH/K1일보완성중담화-전대반응득도3-전-1H-필서병[3,4-b]필진,총수솔약31%.
3-Iodo-1H-pyrazolo [3,4-b] pyrizine was synthesized from 2-cyanopyrazine and thionyl chloride to give 3-chloro-2-cyanopyrazine, which was subjected to cyclization with hydrazine hydrate, followed by diazotization and iodination by NaNO_2/p-TsOH/KI with an overall yield of about 31%.