Cyclopropyl alkenyl amide derivative and synthesizing method thereof
A technology of cyclopropenamide and derivatives, which is applied in chemical instruments and methods, formation/introduction of mercapto/thioether groups, preparation of organic compounds, etc., can solve the problem of weak atom economy, numerous preparation steps, raw materials Problems such as activation are required to achieve the effects of wide applicability, cheap and easy-to-obtain preparation raw materials, and good stereoselectivity
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Embodiment 1
[0047]
[0048] Weigh 4a (123.5mg, 0.5mmol) and iodobenzene acetate (193.3mg, 0.6mmol) into a 25mL Schlenk reaction flask, add 5mL of DCE solvent under air, and stir the reaction at 25°C for 2 hours. After the reaction, the volatile components were removed under reduced pressure, and then separated by silica gel column chromatography (eluent was petroleum ether (60-90°C) / ethyl acetate, v / v=20:1) to obtain the white solid target Product 1a (112.9 mg, yield 74%). The target product was confirmed by NMR and high-resolution mass spectrometry.
Embodiment 2
[0050] The reaction steps and operations are the same as in Example 1, except that the solvent is water. The reaction was stopped, and the target product 1a (50.3 mg, yield 33%) was obtained after post-processing.
Embodiment 3
[0052] The reaction steps and operations are the same as in Example 1, except that the temperature is 80°C. The reaction was stopped, and the target product 1a (57.9 mg, yield 38%) was obtained after post-processing.
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Abstract
Description
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Application Information
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