Alpha-alkylating method of methyl ketone
A technology for alkylation and methyl ketones, which is applied in the field of α-alkylation of methyl ketones, to achieve the effects of reduced synthesis costs, good research and industrial application prospects, and easy operation of the reaction
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Embodiment 1
[0020] Reaction of benzyl alcohol with acetophenone
[0021]
[0022] Under nitrogen protection, benzyl alcohol (6.0 mmol, 3.0 equiv.), acetophenone (2.0 mmol, 1.0 equiv.), and NaOH (1.2 mmol, 60 mol%) were sequentially added to a 20 mL Schlenk reaction tube. The reaction mixture was heated to 120°C and stirred for 24 hours. The reaction was quenched with ethyl acetate, the reaction mixture was washed successively with dilute hydrochloric acid, saturated brine, and water, and then washed with MgSO 4 Dry, filter, and concentrate. The product was obtained by flash column chromatography with a GC yield of 99%, a separation yield of 86%, and a product selectivity of 93 / 7. 1 HNMR(500MHz, CDCl 3 ): δ 7.29-7.13 (m, 10H), 4.59-4.56 (m, 1H), 2.71-2.56 (m, 2H), 2.38 (b, 1H), 2.09-1.93 (m, 2H). 13 C NMR(125.4MHz, CDCl 3 ): δ144.5, 141.7, 128.34, 128.33, 128.26, 127.4, 125.8, 125.7, 73.6, 40.3, 31.9. MS (EI): m / z (%) 212(9), 194(20), 107(100 ), 92(20), 91(22), 79(57), 78(10), 77(28), 51(7)....
Embodiment 2
[0024] Reaction of benzyl alcohol with (4-methyl)acetophenone
[0025]
[0026] Under nitrogen protection, benzyl alcohol (6.0 mmol, 3.0 equiv.), (4-methyl)acetophenone (2.0 mmol, 1.0 equiv.), and NaOH (1.2 mmol, 60 mol%) were sequentially added to a 20 mL Schlenk reaction tube. The reaction mixture was heated to 120°C and stirred for 24 hours. The reaction was quenched with ethyl acetate, the reaction mixture was washed successively with dilute hydrochloric acid, saturated brine, and water, and then washed with MgSO 4 Dry, filter, and concentrate. The product was obtained by flash column chromatography with a GC yield of 99%. 1 H NMR(500MHz, CDCl 3 ): δ 7.28-7.14 (m, 9H), 4.64-4.61 (m, 1H), 2.75-2.61 (m, 2H), 2.34 (s, 3H), 2.14-1.96 (m, 2H), 1.92 (b , 1H). 3 CNMR(125.4MHz, CDCl 3 ): δ141.9, 141.6, 137.3, 129.2, 128.5, 128.4, 125.9, 125.8, 73.7, 40.4, 32.1, 21.1. MS (EI): m / z (%) 226(10), 209(3), 208 (15), 121(100), 93(36), 92(10), 91(35), 77(22), 65(9), 51(4).
Embodiment 3
[0028] Reaction of benzyl alcohol with (4-methoxy)acetophenone
[0029]
[0030] Under nitrogen protection, add benzyl alcohol (6.0 mmol, 3.0 equiv.), (4-methoxy)acetophenone (2.0 mmol, 1.0 equiv.), and NaOH (1.2 mmol, 60 mol%) to a 20 mL Schlenk reaction tube in sequence . The reaction mixture was heated to 120°C and stirred for 24 hours. The reaction was quenched with ethyl acetate, the reaction mixture was washed successively with dilute hydrochloric acid, saturated brine, and water, and then washed with MgSO 4 Dry, filter, and concentrate. The product was obtained by flash column chromatography with a GC yield of 99% and a product selectivity of 86 / 14. 1 H NMR(500MHz, CDCl 3 ): δ7.34-7.15 (m, 7H), 6.87-6.85 (m, 2H), 4.61-4.58 (m, 1H), 3.78 (s, 3H), 2.73-2.58 (m, 2H), 2.13-1.95 (m, 2H), 2.10 (b, 1H). 13 C NMR(125.4MHz, CDCl 3 ): δ 159.0, 141.8, 136.7, 128.4, 128.3, 127.2, 125.8, 113.8, 73.4, 55.2, 40.3, 32.1. MS (EI): m / z (%) 242(7), 224(4), 137 (100), 135(6), 109(20), 94(9...
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