Method for synthesizing substituted amino carboxylic acid by ugi reaction
A technology of aminocarboxylic acid and Uji reaction, which is applied in the field of synthesizing substituted aminocarboxylic acids by Uji reaction, which can solve the problems of harsh reaction conditions and low industrialization level, and achieve the effect of reasonable selection of reaction process and avoiding low yield
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Embodiment 1
[0011] 1 Preparation of dipeptide protected by tert-butyl group:
[0012] Add anhydrous methanol (100ml) to a dry 100ml round-bottomed flask, then add 4-cyanobenzaldehyde (1g, 7.63mmol), replace nitrogen in the reaction flask three times, and slowly add 3-Methylbenzylamine (0.925 g, 7.63 mmol) kept the reaction temperature not higher than 10 °C. After the feeding is completed, the solution turns yellow. After stirring and reacting for 1 hour at 10°C, 2-fluoro-5-methylbenzoic acid (1.18g, 7.63mmol) and tert-butylisocyanate (0.641g, 7.63mmol) are sequentially added under nitrogen protection. ), keep the reaction temperature not higher than 10°C, after feeding is completed, the reaction solution is raised to room temperature and stirred for 24 hours. Until TLC (petroleum ether / ethyl acetate=5:1) detected that the starting material disappeared, the reaction was complete. The reaction solution was spin-dried under reduced pressure. The product 1 (3.32 g, 7.04 mmol) was obtained ...
Embodiment 2
[0019] 1 Preparation of dipeptide protected by tert-butyl group:
[0020] Add anhydrous methanol (100ml) to a dry 100ml round-bottomed flask, then add 4-cyanobenzaldehyde (1g, 7.63mmol), replace nitrogen in the reaction flask three times, and slowly add 3-Methylbenzylamine (0.925 g, 7.63 mmol) kept the reaction temperature not higher than 10 °C. After the feeding is completed, the solution turns yellow. After stirring and reacting for 1 hour at 10°C, 2-fluoro-5-methylbenzoic acid (1.18g, 7.63mmol) and tert-butylisocyanate (0.641g, 7.63mmol) are sequentially added under nitrogen protection. ), keep the reaction temperature not higher than 10°C, after feeding is completed, the reaction solution is raised to room temperature and stirred for 24 hours. Until TLC (petroleum ether / ethyl acetate=5:1) detected that the starting material disappeared, the reaction was complete. The reaction solution was spin-dried under reduced pressure. The product 1 (3.32 g, 7.04 mmol) was obtained ...
Embodiment 3
[0027] 1 Preparation of dipeptide protected by tert-butyl group:
[0028] Add anhydrous methanol (100ml) to a dry 100ml round-bottomed flask, then add 4-cyanobenzaldehyde (1g, 7.63mmol), replace nitrogen in the reaction flask three times, and slowly add 3-Methylbenzylamine (0.925 g, 7.63 mmol) kept the reaction temperature not higher than 10 °C. After the feeding is completed, the solution turns yellow. After stirring and reacting for 1 hour at 10°C, 2-fluoro-5-methylbenzoic acid (1.18g, 7.63mmol) and tert-butylisocyanate (0.641g, 7.63mmol) are sequentially added under nitrogen protection. ), keep the reaction temperature not higher than 10°C, after feeding is completed, the reaction solution is raised to room temperature and stirred for 24 hours. Until TLC (petroleum ether / ethyl acetate=5:1) detected that the starting material disappeared, the reaction was complete. The reaction solution was spin-dried under reduced pressure. The product 1 (3.32 g, 7.04 mmol) was obtained ...
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