Unlock instant, AI-driven research and patent intelligence for your innovation.
A kind of preparation method of isavuconazole
What is Al technical title?
Al technical title is built by PatSnap Al team. It summarizes the technical point description of the patent document.
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
View PDF4 Cites 0 Cited by
Summary
Abstract
Description
Claims
Application Information
AI Technical Summary
This helps you quickly interpret patents by identifying the three key elements:
Problems solved by technology
Method used
Benefits of technology
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
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more
Image
Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
Click on the blue label to locate the original text in one second.
Reading with bidirectional positioning of images and text.
Smart Image
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.
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More
PUM
Login to View More
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
the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More
Application Information
Patent Timeline
Application Date:The date an application was filed.
Publication Date:The date a patent or application was officially published.
First Publication Date:The earliest publication date of a patent with the same application number.
Issue Date:Publication date of the patent grant document.
PCT Entry Date:The Entry date of PCT National Phase.
Estimated Expiry Date:The statutory expiry date of a patent right according to the Patent Law, and it is the longest term of protection that the patent right can achieve without the termination of the patent right due to other reasons(Term extension factor has been taken into account ).
Invalid Date:Actual expiry date is based on effective date or publication date of legal transaction data of invalid patent.
Login to View More 
Login to View More 
