3-substituted 3-vinyl-2-hydroxy-1-aryl acetone and synthetic method thereof
A technology of aryl acetone and synthesis method, which is applied in the field of synthesis of chiral compounds, can solve the problems of poor reaction selectivity, unfavorable drug synthesis and screening, increased economic cost and time cost, etc., and achieves mild reaction conditions, shortened process, and easy synthesis low cost effect
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Embodiment 1
[0030] 1.8 mg of L1 ligand was added to a 5 ml reaction flask, and 0.3 ml of toluene and 12.5 μl of diethyl zinc solution (0.0125 mmol) were added thereto under nitrogen protection, and stirred at 25° C. for 30 minutes to obtain a zinc catalyst.
[0031] Add 3.4mg (1,5-cyclooctadiene) iridium chloride dimer and 5.4mg (R,R,R)-L6 ligand to a 10ml reaction bottle, and add 0.5ml Tetrahydrofuran and 0.5ml of n-propylamine were stirred at 50°C for 30 minutes, and the solvent was concentrated and spin-dried to obtain an iridium catalyst.
[0032] Under nitrogen protection conditions, 48.0mg cinnamyl methyl carbonate, 40.8mg 2-hydroxy-1-acetophenone, 100mg Molecular sieves, zinc catalyst, iridium catalyst and 2ml tetrahydrofuran were added into a 10ml reaction flask, and stirred at 25°C for 12 hours. The reaction solution was concentrated and spin-dried to dry the solvent, and passed through a silica gel column to obtain a purified product with a yield of 41%, a dr value of 1:1, and...
Embodiment 2
[0035]2.5 mg of L2 ligand was added to a 5 ml reaction bottle, and 0.3 ml of toluene and 12.5 μl of diethyl zinc solution (0.0125 mmol) were added thereto under nitrogen protection, and stirred at 25° C. for 30 minutes to obtain a zinc catalyst.
[0036] Add 3.4mg (1,5-cyclooctadiene) iridium chloride dimer and 5.4mg (R,R,R)-L6 ligand to a 10ml reaction bottle, and add 0.5ml Tetrahydrofuran and 0.5ml of n-propylamine were stirred at 50°C for 30 minutes, and the solvent was concentrated and spin-dried to obtain an iridium catalyst.
[0037] Under nitrogen protection conditions, 48.0mg cinnamyl methyl carbonate, 40.8mg 2-hydroxy-1-acetophenone, 100mg Molecular sieves, zinc catalyst, iridium catalyst and 2ml tetrahydrofuran were added into a 10ml reaction flask, and stirred at 25°C for 12 hours. The reaction solution was concentrated and spin-dried to dry the solvent, and passed through a silica gel column to obtain a purified product with a yield of 49%, a dr value of 1:1, and...
Embodiment 3
[0039] 3.3 mg of L3 ligand was added to a 5 ml reaction bottle, and 0.3 ml of toluene and 12.5 μl of diethyl zinc solution (0.0125 mmol) were added thereto under nitrogen protection, and stirred at 25° C. for 30 minutes to obtain a zinc catalyst.
[0040] Add 3.4mg (1,5-cyclooctadiene) iridium chloride dimer and 5.4mg (R,R,R)-L6 ligand to a 10ml reaction bottle, and add 0.5ml Tetrahydrofuran and 0.5ml of n-propylamine were stirred at 50°C for 30 minutes, and the solvent was concentrated and spin-dried to obtain an iridium catalyst.
[0041] Under nitrogen protection conditions, 48.0mg cinnamyl methyl carbonate, 40.8mg 2-hydroxy-1-acetophenone, 100mg Molecular sieves, zinc catalyst, iridium catalyst and 2ml tetrahydrofuran were added into a 10ml reaction flask, and stirred at 25°C for 12 hours. The reaction solution was concentrated and spin-dried to dry the solvent, and the purified product was obtained by passing through a silica gel column with a yield of 44%, a dr value o...
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