Method for synthesizing anti-AIDS pharmaceutical efavirenz

Abstract

The invention discloses a method of synthesizing efavirenz which is an anti-AIDS medicine. The synthesizing steps are that: 4-chloro-2-trifluoroethylanilid is taken as raw material, after an h (hydrogen) on N being protected by protective group and the function of a ligand, the raw material is reacted with the substitute of cyclopropyl acetylene, thereby acquiring a chiral intermediate which is ring-closured and deprotected to obtain efavirenz product. The synthesizing method has the advantages that the cost is low, the reaction route is safe and environment protective and the chiral ee value of the product is high, etc.

Description

technical field [0001] The invention relates to a drug synthesis method, in particular to a synthesis method of the anti-AIDS drug efavirenz. Background technique [0002] As an anti-HIV drug, Efavirenz is mainly used in combination with other anti-HIV drugs to form a "cocktail therapy" to treat AIDS. At present, cocktail therapy is widely used in the treatment of AIDS. Such drugs have received increased attention from the medical industry as the number of people living with HIV increases globally. Many literatures have reported the synthesis method of efavirenz before. In literature reports, in the step of synthesizing chiral products, the ligand of desmethylephedrine is basically used. This ligand is the precursor of synthetic drugs, which has high risk and high cost, and the industrialization effect is not ideal [Synthetic Communications.27(24), 1997.4373-4384, Angew.Chem.Int.Ed.1999.38(5).711-713, J.Org.Chem.63(23).1998.8536-8543, J.Med.Chem.2000.43 .2019-2030]. The...

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Problems solved by technology

In literature reports, in the step of synthesizing chiral products, the ligand of desmethylephedrine is basically used. This ligand is the precursor of synthetic drugs, which has high risk and high cost, and the industrialization effect is not ideal [Synthetic Communications.27(24), 1997.4373-4384, Angew.Chem.Int.Ed.1999.38(5).711-713, J.Org.Chem.63(23).1998.8536-8543, J.Med.Chem.2000.43 .2019-2030]

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