本研究成功开发了异氰酸酯与原位生成的偶氮烯烃在碱促进下的[4 + 1]环加成反应。在温和的反应条件下,该反应提供了高效实用的获得吡唑-5-甘氨酸衍生物的途径,反应具有良好到极好的产率。异氰酸酯在反应中作为C1合子,其氰基碳参与了环...本研究成功开发了异氰酸酯与原位生成的偶氮烯烃在碱促进下的[4 + 1]环加成反应。在温和的反应条件下,该反应提供了高效实用的获得吡唑-5-甘氨酸衍生物的途径,反应具有良好到极好的产率。异氰酸酯在反应中作为C1合子,其氰基碳参与了环加成过程。MTT试验表明,该反应产物具有抑制HeLa癌细胞增殖的活性。A base-promoted [4 + 1] annulation reaction of isocyanoacetates with in situ generated azoalkenes was successfully developed. The reaction provided efficient and practical access to pyrazole-5-glycine derivatives with good to excellent yields under mild reaction conditions. Isocyanoacetates served as C1 synthon and its cyano carbon participated in the annulation in this protocol. The MTT assay shows that the product exhibits the activity of an inhibitory effect on proliferation on HeLa cancer cell line.展开更多
文摘本研究成功开发了异氰酸酯与原位生成的偶氮烯烃在碱促进下的[4 + 1]环加成反应。在温和的反应条件下,该反应提供了高效实用的获得吡唑-5-甘氨酸衍生物的途径,反应具有良好到极好的产率。异氰酸酯在反应中作为C1合子,其氰基碳参与了环加成过程。MTT试验表明,该反应产物具有抑制HeLa癌细胞增殖的活性。A base-promoted [4 + 1] annulation reaction of isocyanoacetates with in situ generated azoalkenes was successfully developed. The reaction provided efficient and practical access to pyrazole-5-glycine derivatives with good to excellent yields under mild reaction conditions. Isocyanoacetates served as C1 synthon and its cyano carbon participated in the annulation in this protocol. The MTT assay shows that the product exhibits the activity of an inhibitory effect on proliferation on HeLa cancer cell line.
