Study Of The Synthesis Of 2-aminobutanol

2-aminobutanol is the key intermediate for the synthesis of ethambutol, and ethambutol hydrochloride was used as antituberculosis drugs. Ethambutol hydrochloride was used as first-line antituberculosis drugs, applicable to all types of pulmonary and extrapulmonary tuberculosis, the drug had a stronger inhibitory effect on tuberculosis, but is not obvious in other bacteria, no cross-resistance with other antituberculosis drugs. In foreign countries, the synthesis of ethambutol hydrochloride has done in-depth study, but the domestic research started relatively late, leading to the drugs long-term dependence on imported. So it is necessary to study the synthesis of ethambutol hydrochloride.In this thesis, using butyraldehyde and 2- aminobutyric acid as raw material, racemic 2- aminobutanol have been synthesized.2-aminobutanol was synthesized through halogenation, reduction and ammonolysis reaction from butyraldehyde. The yield reached to 74.5%, according to butyraldehyde. The content was up to 99%. And the route of reaction was studied, we have chosen a halogenating reaction catalyst, solvent and halogen source. Under the optimum conditions, the intermediate 2- chloro butyraldehyde yield can reach 92%. Hydrogen transfer reduction reaction, using aluminum isopropoxide as catalyst, the product 2- chloro butyl alcohol yield was 94%. Finally, the ammonolysis reaction were carried out under different conditions, and the product 2-aminobutanol was got, the yield was 89.6% and the purity was 99%.Using racemic 2-aminobutyric acid as starting material, 2-aminobutanol was synthesized by esterification, amino protection, hydrogenation and deprotection of amino reaction. And we also discussed the factors influencing the yield of the reaction. The total yield was 62.7%, the purity of product was 99.2%.