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A kind of preparation method of isavuconazole

A technology of isavuconazole and triazole, applied in the field of medicine, can solve the problems of rising cost, reduced yield, numerous process steps, etc., and achieve the effects of reducing reaction steps, improving yield and reducing cost

Inactive Publication Date: 2018-03-27
苏州金点生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the existing preparation method of isavuconazole sulfate, there are many process steps, which means that the yield is reduced and the cost is significantly increased

Method used

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  • A kind of preparation method of isavuconazole

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] The invention provides a preparation method of isavuconazole, such as figure 1 As shown, it includes the following steps:

[0023] (a) Add 1 mol of difluorophenylacetyl chloride, 1.2 mol of triazole, 0.15 mol of CuI, 1.5 mol of potassium carbonate and 0.8 L of DMF (N,N-dimethylformamide) into the reaction kettle, and heat up to 80°C The reaction was stirred for 10 hours, and TLC (thin layer chromatography) detected that the reaction was complete; the filtrate was filtered and concentrated under reduced pressure to recover DMF, and the residue was recrystallized with ethyl acetate to obtain an off-white solid, the first product, with a yield of 73 %;

[0024] (b) In the three-necked reaction flask, add 4mol propionitrile, 0.1mol catalyst (comprising 0.05mol C-9 primary amine cinchona base, chemical formula is And 0.05mol cuprophylline, the chemical formula is ), 0.1mol benzoic acid and 0.5L N,N-dimethylacetamide (DMA), cooled to -10°C, stirred and added dropwise 0.3...

Embodiment 2

[0028] This embodiment provides a preparation method of isavuconazole, the preparation steps of which are basically the same as those in Example 1, the difference is that in step (b), no benzoic acid is added, and the yield of the final second product is 75% %, dr. is 95:5.

Embodiment 3

[0030] This embodiment provides a preparation method of isavuconazole, the preparation steps of which are basically the same as those in Example 1, except that in step (b), the C-9 primary amine cinchonaline and copper-colored tree in the catalyst The molar ratio of the base is 5:1, the yield of the final second product is 76%, and the dr. is 95:5.

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Abstract

The invention relates to a catalyst. The catalyst is used for carrying out addition reaction on a substance shown in the description and propionitrile to generate a product shown in the description, wherein the product is a mixture composed of C-9 primary amine cinchona alkaloid with a formula shown in the description and cupreine with a formula shown in the description; the mol ratio of the C-9 primary amine cinchona alkaloid to the cupreine is 1 to 1. By adopting the catalyst, asymmetric addition of the propionitrile is realized and existing defects are broken through.

Description

technical field [0001] The invention belongs to the field of medicines and relates to isavuconazole, in particular to a preparation method of isavuconazole and isavuconazole prepared therefrom. Background technique [0002] In the past 20 years, due to the extensive use of hematopoietic stem cell transplantation, solid organ transplantation, tumor chemotherapy, broad-spectrum antibiotics, glucocorticoids, and immunosuppressants, the prevalence of invasive fungal infections has shown a significant upward trend. Invasive fungal infections are mainly caused by Candida and Aspergillus, and the susceptible population is immunocompromised patients, which mostly occur in the fields of blood, ICU, transplantation, respiratory and infection, among which hematology patients, such as bone marrow transplantation, leukemia Patients with lymphoma and lymphoma accounted for about 61%, infection and respiratory patients accounted for about 17%, mainly concentrated in patients with AIDS, res...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D417/06C07D405/14
CPCB01J31/0244B01J35/0006B01J2231/32C07B53/00C07B2200/07C07D249/08C07D405/14C07D417/06
Inventor 刘元超倪润炎孙伟娅刘可王伟
Owner 苏州金点生物科技有限公司
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