Method used for preparing Lopinavir using one-pot method

Abstract

The invention discloses a method used for preparing lopinavir using one-pot method. According to the method, under certain organic solvent conditions, (2S)-(1-Tetrahydropyramid-2-one)-3-methylbutanoicacid is reacted with thionyl chloride so as to obtain (2S)-(1-Tetrahydropyramid-2-one)-3-methyl butyryl chloride; a weak base acid binding agent and N-[(1S,2S,4S)-4-amino-2-hydroxy-5-phenyl-1-(phenylmethyl)pentyl]-2-(2,6-dimethylphenoxy)acetamide are added into an obtained reaction system for amidation reaction; after amidation reaction, an obtained product is subjected to post-treatment so as toobtain lopinavir finished product. According to the method, on-pot method is adopted, the process is simple, production period is short, the finial products can be separated and purified easily, synthesis yield is high, the method is economical and is high in feasibility, and is suitable for industrialized production.

Description

technical field [0001] The invention relates to a method for preparing lopinavir by a one-pot method, which belongs to the technical field of medicine. Background technique [0002] Lopinavir, chemical name: (2S)-N-[(2R,4S,5S)-5-[[2-(2,6-Dimethylphenoxy)acetyl]amino]-4-hydroxy -1,6-diphenyl-hex-2-yl]-3-methyl-2-(2-oxo-1,3-diazacyclohex-1-yl)butanamide, its structure is as follows Shown: [0003] [0004] Lopinavir is an HIV-1 and HIV-2 protease inhibitor, which can be combined with low-dose ritonavir to improve its pharmacokinetic properties. Lopinavir combined with low-dose ritonavir compound tablet was approved by the United States in 2000 Approved by the Food and Drug Administration for marketing, it has reliable curative effect, few side effects, and is less affected by food. It is currently used as a first-line or second-line treatment drug against human immunodeficiency virus, and plays an important role in the antiviral treatment of HIV patients who have failed i...

AI Technical Summary

Problems solved by technology

[0012] Although the product quality and yield of method 3 are acceptable, the step of activated ester reaction is increased, and the operation and post-treatment are cumbersome. Considering the cost, it is not suitable for industrial production;

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