SIMPLIFIED PROCEDURE FOR OBTAINING DARUNAVIR Russian patent published in 2021 - IPC C07D493/04 

Abstract RU 2745740 C2

FIELD: medicine.

SUBSTANCE: invention relates to a method for producing (3R, 3aS, 6aR) -hexahydrofuro [2,3-b] furan-3-yl ester [(1S, 2R) -3 - [[(4-aminophenyl) sulfonyl] (2- methylpropyl) amino] -2-hydroxy-1- (phenylmethyl) -propyl] -carbamic acid (darunavir), which consists in the interaction of 2,5-dioxo-1-pyrrolidinyl [(3R, 3aS, 6aR) -hexahydrofuro [2, 3 – b] furan – 3 – yl] carbonic acid ester with 4 – amino – N - [(2R, 3S) –3 – amino – 2 – hydroxy – 4 – phenylbutyl] –N– (2 – methylpropyl) –benzenesulfamide in ethanol as a solvent when the reaction mixture is heated at a temperature from 30°C to the reflux temperature.

EFFECT: new method has been developed for obtaining darunavir with a high output, which allows darunavir to be isolated immediately in the form of monoethanolate that is used in medicine to treat Human Immunodeficiency Virus Type 1 (HIV-1).

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RU 2 745 740 C2

Authors

Stappers, Alfred Elisabeth

Lang, Yolande Lydia

Robinson, Shane Barry

Dates

2021-03-31Published

2017-11-16Filed