A kind of preparation method of emtricitabine

Abstract

The invention discloses a preparation method of emtricitabine. Purified to obtain pure 5S-(5'-fluorocytosinyl-1')-1,3-oxathiolane-2-ethoxycarbonyl-(1'R, 2'S, 3'R)-menthyl ester ; Slough the chiral auxiliary agent L Menthol under the condition of weak base and solvent to obtain product emtricitabine. The starting materials required by the present invention are cheap and easy to obtain, the reaction conditions are mild, the utilization rate of atoms is high, the operation process is simple, the reagents used are green and environmentally friendly, the obtained product has high chemical purity, reaches the pharmaceutical standard, and is suitable for industrial production of emtricitabine .

Description

technical field

[0001] The invention relates to the technical field of drug synthesis. Specifically relates to a preparation method of emtricitabine. Background technique

[0002] Emtricitabine (FTC) was developed by Gilead Science of the United States and was first launched in the United States in July 2003. Its chemical name is: (2R,5S)-4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-2(1H)-pyrimidine ketone. It is a nucleoside reverse transcriptase inhibitor, which has good curative effect on the treatment of human immunodeficiency virus (HIV) and hepatitis B virus (HBV). Its mechanism of action is that after oral administration, it is phosphorylated into 5'-triphosphate with cell activity, and 5'-triphosphate enters the main chain of viral DNA and binds to the main chain, leading to chain termination, thereby inhibiting HIV-1 reverse transcription Enzyme and HBV DNA polymerase activity to achieve the effect of inhibiting the virus.

[0003] At present, many ...

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