- Synthesis process of N-amino-3-azabicyclo [3, 3, 0] octane hydrochloride
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The invention provides a synthesis process of N-amino-3-azabicyclo [3, 3, 0] octane hydrochloride, and relates to the technical field of gliclazide intermediate synthesis. The synthesis process comprises the following steps: heating, dehydrating and cyclizing 2-carbamoyl amine cyclopentanecarboxylate serving as a raw material under the catalysis of an acid catalyst until no water is generated, adding toluene, refluxing and dissolving, and carrying out post-treatment to obtain 1, 2-cyclopentane dicarboximide; reacting the 1, 2-cyclopentane dicarboximide with chloramine under an alkaline condition, and carrying out post-treatment to obtain N-amino-1, 2-cyclopentane dicarboximide; and reducing the amino-1, 2-cyclopentane dicarboximide in the presence of sodium borohydride/aluminum trichloride and an organic solvent, and performing post-treatment to obtain the product. According to the present invention, the three-step synthesis is performed through the catalytic cyclization reaction, the nucleophilic substitution reaction and the reduction reaction, the raw materials are cheap and easily available, the high toxicity product is not generated, the harsh reaction condition is not required, the yield and the purity of each step are high, and the method is suitable for the large-scale industrial production.
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Paragraph 0017; 0027; 0029; 0032; 0034; 0037; 0039; 0042;
(2021/05/29)
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