Preparation method of chiral β-substituted-α, β-unsaturated amino alcohol compounds
An amino alcohol, unsaturated technology, applied in the preparation of amino hydroxyl compounds, organic compounds, carbamic acid derivatives, etc., to achieve the effect of mild conditions, good application effect, and easy operation
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Embodiment 1、2
[0038] Embodiment 1, 2a (R=C 6 h 5 ) preparation
[0039]In a 10mL reaction tube, add phosphine ligand L4a (5.8mg, 0.012mmol) and allyl palladium chloride (1.8mg, 0.005mmol), the system passed through the vacuum line, replaced with nitrogen for 3 times, and added freshly distilled tetrahydrofuran 1 mL, the solution was stirred at 20°C for 1 hour, and at the same time, in another 10 mL reaction tube, β-substituted-α, β-unsaturated carbonate 1a (38 mg, 0.2 mmol) and potassium phthalimide ( 41.7mg, 0.225mmol), the system passed through the vacuum line, replaced with nitrogen 3 times, added freshly distilled tetrahydrofuran 1mL, and the solution was stirred at 20°C for 1 hour. The coordinated catalyst was withdrawn with a syringe and injected into the reaction tube containing the substrate and nucleophile, stirred at 20°C for 8 hours, quenched with saturated ammonium chloride, and extracted with ethyl acetate (20mL×2), the organic phase After drying with anhydrous sodium sul...
Embodiment 2、2
[0040] Embodiment 2, 2b (R=2-CH 3 C 6 h 4 ) preparation
[0041] In a 10mL reaction tube, add phosphine ligand L4a (5.8mg, 0.012mmol) and allyl palladium chloride (1.8mg, 0.005mmol), the system passed through the vacuum line, replaced with nitrogen for 3 times, and added freshly distilled tetrahydrofuran 1 mL, the solution was stirred at 25°C for 1 hour, and at the same time, in another 10 mL reaction tube, β-substituted-α, β-unsaturated carbonate 1b (40.8 mg, 0.2 mmol) and potassium phthalimide were added (41.7mg, 0.225mmol), the system was replaced with nitrogen three times through a vacuum line, 1 mL of freshly distilled tetrahydrofuran was added, and the solution was stirred at 25°C for 1 hour. The coordinated catalyst was withdrawn with a syringe and injected into the reaction tube containing the substrate and nucleophile, stirred at 25°C for 12 hours, quenched with saturated ammonium chloride, and extracted with ethyl acetate (20mL×2), the organic phase After dry...
Embodiment 3、2
[0042] Embodiment 3, 2c (R=3-CH 3 C 6 h 4 ) preparation
[0043] In a 10mL reaction tube, add phosphine ligand L4a (5.8mg, 0.012mmol) and allylpalladium chloride (1.8mg, 0.005mmol), the system passed through the vacuum line, replaced with nitrogen for 3 times, and added freshly distilled benzene 1 mL, the solution was stirred at 30°C for 1 hour, and at the same time in another 10 mL reaction tube, β-substituted-α, β-unsaturated carbonate 1c (40.8 mg, 0.2 mmol) and potassium phthalimide were added (41.7 mg, 0.225 mmol), the system was replaced with nitrogen three times through a vacuum line, 1 mL of freshly distilled benzene was added, and the solution was stirred at 30° C. for 1 hour. The coordinated catalyst was drawn out with a syringe and injected into the reaction tube containing the substrate and nucleophile, stirred at 30°C for 10 hours, quenched with saturated ammonium chloride, and extracted with ethyl acetate (20mL×2), the organic phase After drying with anhyd...
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