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Preparation method of ritonavir

A technology for ritonavir and compound, applied in the field of preparation of ritonavir, can solve problems such as unfavorable scale-up production, low yield, high price, etc., and achieves low cost, easy large-scale production, and good application prospect Effect

Pending Publication Date: 2019-02-22
贵州永诺菲特生物制药有限公司
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Problems solved by technology

The p-nitrophenyl chloroformate used in this method is very active, so that the yield in the first two steps is not high, only 54%; the condensing agent used in the final condensation step is EDCI, which is expensive and unfavorable for large-scale production

Method used

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  • Preparation method of ritonavir
  • Preparation method of ritonavir
  • Preparation method of ritonavir

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Embodiment

[0043] Such as figure 1 Shown, the preparation method of a kind of ritonavir of the present invention comprises the following steps:

[0044] Step 1, the preparation of compound III, the reaction scheme is as follows:

[0045]

[0046] a. Add (2-isopropylthiazol-4-yl)-nitrogen-methylmethylamine 50.0 g (0.294 mol, 1.0 eq), (S)-3-methyl-2-[(2,2,2 -Trichloroethoxy)formamide]butyric acid 86.0 g (0.294 mol, 1.0 eq), triethylamine 38.6 g (0.382 mol, 1.3 eq) and tetrahydrofuran 250 mL were added to the reaction flask, and the temperature was raised to 50-60°C;

[0047] b, start the reaction until the reaction 6h to the disappearance of raw materials;

[0048] c. After the reaction is completed, cool down to room temperature, pour into 500 mL of 1N hydrochloric acid, and extract with 250 mL of ethyl acetate × 2;

[0049] d. Combine the organic phases, wash with 300 mL of water, and then wash with 300 mL of saturated brine;

[0050] e. Concentrate under reduced pressure to dryne...

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Abstract

The invention relates to the technical field of medicine, in particular to a preparation method of ritonavir. According to the preparation method of the ritonavir, (2-isopropyl thiazole-4-yl)-nitrogen-methyl methylamine is taken as a raw material, and the ritonavir is synthesized through a three-step reaction; a urea bond is built by trichloroethanol chloroformate, paratoluensulfonyl chloride which is cheap and easy to obtain is adopted as a condensing agent for amide, the ritonavir is synthesized with the high yield, and the yield of the ritonavir is 79%; and compared with an existing preparation method, the preparation method has the advantages of low cost, environment friendliness, easy scale production and the like, and has good application prospects.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a preparation method of ritonavir. Background technique [0002] At present, the design of anti-HIV drugs is mainly aimed at the three key enzymes in the HIV replication cycle, namely reverse transcriptase, protease, integrase, and HIV invasion process. According to the different drug targets, it can be divided into six categories, namely: nucleoside reverse transcriptase inhibitors (NRTIs), non-nucleoside reverse transcriptase inhibitors (NNRTIs), protease inhibitors (PIs), entry inhibitors ( EIs), integrase inhibitors (IIs) and CCR5 receptor antagonists, etc. In 1987, the first anti-HIV drug Zidovudine (AZT), which belongs to nucleoside reverse transcriptase inhibitors, was launched on the market. Saquinavir is the world's first approved protease inhibitor. It was developed by Roche in 1995 and approved by the FDA. Good results have been obtained, and thus the era of combin...

Claims

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Application Information

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IPC IPC(8): C07D277/28
CPCC07D277/28
Inventor 冉刚任旭张毅宁兆伦周钟
Owner 贵州永诺菲特生物制药有限公司
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