1-aryl-5-aminotetrazole compound and preparation method thereof
A technology of aminotetrazole and nitrogen-based tetrazole, which is applied in the direction of organic chemistry, can solve the problems of no reaction selectivity, poor atom economy, troublesome raw material synthesis, etc., and achieve easy operation, convenient post-processing, and stability good sex effect
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Embodiment 1
[0034] In a 50 ml reaction bottle, add in sequence, 665 mg (5 mmol) 4-methoxybenzene isonitrile, 3.61 g (12.5 mmol) hypervalent iodine azide reagent, 181 mg (1 mmol) anhydrous copper acetate , 325 mg (1 mmol) of cesium carbonate, then added 30 ml of anhydrous DMF under nitrogen protection, and stirred at 25°C for 12 hours. After the reaction was finished, the solvent was removed and purified by column chromatography to obtain 542 mg of light yellow solid product with a yield of 50%, and the molecular formula was:
[0035]
[0036] H NMR (500 MHz, CDCl 3 ) chemical shift (unit ppm) 7.51 (d, J = 9.0 Hz, 2H), 7.01 (d, J = 9.0 Hz, 2H), 3.85 (s, 3H).
[0037] C NMR spectrum (125 MHz, CDCl 3 ) chemical shift (unit ppm) 160.5, 151.4 , 125.5, 124.3 , 114.7 , 55.6 .
[0038] Infrared Spectrum (KBr): n max 3061, 2945, 2843, 2161, 1597, 1523, 1458, 1255, 1193, 1016, 832,784 cm -1
[0039] Melting point: 84-86 o c.
[0040] In the 50 milliliter reaction bottle, add succe...
Embodiment 2
[0046] In a 50 ml reaction bottle, add successively, 900 mg (5 mmol) 4-bromophenylisonitrile, 3.61 g (12.5 mmol) hypervalent iodine azide reagent, 181 mg (1 mmol) anhydrous copper acetate, 325 mg (1 mmol) of cesium carbonate, then added 30 ml of anhydrous DMF under nitrogen protection, and stirred at 25°C for 12 hours. After the reaction, the solvent was removed,
[0047] Separation and purification by column chromatography gave 731.5 mg of a light yellow solid product with a yield of 55%, and the molecular formula was:
[0048]
[0049] H NMR spectrum (500 MHz, CDCl 3 ) chemical shift (unit ppm) 7.67 (d, J = 8.8Hz, 2H), 7.57 (d, J = 8.8 Hz, 2H).
[0050] C NMR spectrum (125 MHz, CDCl 3 ) chemical shift (in ppm) 151.4, 132.9, 131.8, 123.7, 123.7
[0051] Infrared spectrum (KBr): n max 3053, 2923, 2856, 2148, 1596, 1524, 1458, 1321, 1102, 824 cm -1
[0052] Melting point: 110-113 o c.
[0053] In the 50 milliliter reaction bottle, add successively, 726 milligr...
Embodiment 3
[0060] In a 50 ml reaction bottle, add 655 mg (5 mmol) of 2,4-dimethylbenzeneisonitrile, 3.61 g (12.5 mmol) of hypervalent iodine azide reagent, and 181 mg (1 mmol) of anhydrous Copper acetate, 325 mg (1 mmol) cesium carbonate, and then 30 ml of anhydrous DMF were added under nitrogen protection, and stirred at 25°C for 12 hours. After the reaction was finished, the solvent was removed and purified by column chromatography to obtain 645 mg of light yellow solid product with a yield of 60%, and the molecular formula was:
[0061]
[0062] H NMR spectrum (500 MHz, CDCl 3 ) chemical shift (in ppm) 7.18 (s, 1H), 7.14 (d, J = 7.7 Hz, 1H), 7.10 (d, J = 8.0 Hz, 1H), 2.39 (s, 3H), 2.09 (s, 3H).
[0063] C NMR spectrum (125 MHz, CDCl 3 ) chemical shifts (in ppm) 152.9, 141.6, 134.5 , 132.1 , 128.5 , 127.7 , 126.4 , 21.2 , 17.3 .
[0064] Infrared Spectrum (KBr): n max 3065, 2966, 2923, 2854, 2151, 1612, 1523, 1497, 1457, 1254, 1091, 1018, 864, 805 cm -1
[0065] Melting...
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