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Molnupiravir crystal form A and preparation method thereof

A crystal form, cu-k technology, applied in the field of medicine and chemical industry

Inactive Publication Date: 2021-05-11
HANGZHOU CHEMINSPIRE TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

PCT patent WO2019113462A reports the chemical synthesis route of Molnupiravir. The crystal form of Molnupiravir is not reported in the existing patents. During the experimental research, the inventor found that there is a new crystal form A of Molnupiravir. The present invention provides a kind of Molnupiravir The new crystal form A, which provides more options for the application of Molnupiravir

Method used

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  • Molnupiravir crystal form A and preparation method thereof
  • Molnupiravir crystal form A and preparation method thereof
  • Molnupiravir crystal form A and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Add Molnupiravir (1.0g, purity 98.0%) and 5mL of isopropanol into the three-necked flask, stir evenly, then heat up to 55-60°C, stir for 2-3 hours, slowly cool to 0-5°C for crystallization, and keep stirring for 10 After ~16 hours, centrifuge and dry to obtain 0.90 g of Form A (purity 99.8%, yield 91.7%).

[0037] The X-ray powder diffraction data of the crystal form A obtained in this embodiment are shown in Table 1, and its XRPD pattern is as follows figure 1 , and its DSC graph is shown in figure 2 , and its TGA figure is shown in image 3 .

[0038] Table 1

[0039] 2THETA d interval strength% 3.26 27.07 100.00％ 6.52 13.54 6.10％ 9.80 9.02 0.80％ 13.09 6.76 3.20％ 16.38 5.41 3.30％ 17.08 5.19 2.60％ 17.20 5.15 2.70％ 18.10 4.90 1.60％ 19.49 4.55 0.90％ 19.67 4.51 1.20％ 19.90 4.46 0.70％ 20.38 4.35 0.70％ 20.61 4.31 1.20％ 21.33 4.16 3.20％ 23.39 3.80 0.70％ 24.06 3.70...

Embodiment 2

[0041] Add Molnupiravir (1.0g, purity 98.0%) and 5mL of water into a three-necked flask, stir well, then heat up to 55-60°C, stir for 2-3 hours, slowly cool to 0-5°C for crystallization, and keep stirring for 10-16 hours, centrifuged and dried to obtain 0.82 g of Form A (purity 99.5%, yield 83.3%).

[0042] The X-ray powder diffraction data of the crystal form A obtained in this embodiment are shown in Table 2,

[0043] Table 2

[0044]

[0045]

Embodiment 3

[0047]Add Molnupiravir (1.0g, purity 98.0%) and ethyl acetate 3mL into the three-necked flask, stir evenly, then heat up to 55-60°C, stir for 2-3 hours, slowly cool to 0-5°C for crystallization, and keep stirring for 10 After ~16 hours, centrifuge and dry to obtain 0.93 g of Form A (purity 99.6%, yield 94.5%).

[0048] The X-ray powder diffraction data of the crystal form A obtained in this embodiment are shown in Table 3,

[0049] table 3

[0050]

[0051]

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PUM

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Abstract

The invention provides a Molnupiravir crystal form A. An X-ray powder diffraction pattern 2Theta value obtained by Cu-K alpha ray measurement has characteristic peaks at 3.26 + / - 0.2 degrees, 6.52 + / - 0.2 degrees, 13.09 + / -0.2 degrees, 16.38 + / - 0.2 degrees, 21.33 + / - 0.2 degrees and 31.69 + / - 0.2 degrees. The crystal form is simple in preparation process and simple and convenient to operate, has good stability, is easy to store in the production and circulation process, provides a good choice for preparation of pharmaceutical preparations of the crystal form, and has very important significance for drug development.

Description

technical field [0001] The invention belongs to the field of medicine and chemical industry, and in particular relates to a novel antiviral drug Molnupiravir crystal form A and a preparation method thereof. Background technique [0002] Molnupiravir (code-named MK-4482 or EIDD-2801) is a small-molecule cytidine antiviral drug developed by Merck in the United States for oral administration. The drug is a SARS-CoV2 polymerase inhibitor. Studies have confirmed that in animal experiments, Molnupiravir used to treat ferrets infected with SARS-CoV-2 can effectively inhibit the virus and prevent the growth of the new coronavirus within 24 hours, thereby inhibiting the spread of the virus. The team believes that if Molnupiravir works similarly in human trials, COVID-19 patients treated with the oral drug could become non-infectious within a day. At present, Merck has started clinical trials for the treatment of patients with the new coronavirus. Once successful, the market prospec...

Claims

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Application Information

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IPC IPC(8): C07H19/067C07H1/00
CPCC07H19/067C07H1/00C07B2200/13
Inventor 郑旭春张一平付晨晨
Owner HANGZHOU CHEMINSPIRE TECH CO LTD
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