School of Pharmaceutical Sciences, Nanjing Tech University, Nanjing 211816, P. R. China.
School of Food Science and Pharmaceutical Engineering, Nanjing Normal University, Nanjing 210023, P. R. China.
Org Biomol Chem. 2020 Dec 7;18(46):9483-9493. doi: 10.1039/d0ob01958e.
A facile and efficient strategy for the synthesis of 1,4-dihydropyridazines and pyridazines through I2-promoted [4 + 2] cycloaddition of in situ generated azoalkenes with enaminones has been developed. The switch in selectivity is attributed to the judicious choice of different reaction temperatures. The key features of this work include controllable and selective synthesis, good functional group tolerance, good to excellent reaction yields, metal/base-free conditions, and also applicability to one-pot methodology.
通过 I2 促进原位生成的偶氮烯烃与烯胺酮的[4 + 2]环加成反应，开发了一种简便高效合成 1,4-二氢嘧啶和嘧啶的策略。选择性的转变归因于不同反应温度的合理选择。这项工作的关键特点包括可控和选择性合成、良好的官能团耐受性、良好到优秀的反应收率、无金属/碱条件，以及适用于一锅法。
