Al technical title is built by PatSnap Al team. It summarizes the technical point description of the patent document.
The technology of a compound and a basic substance is applied in the field of preparing an antidiabetic drug Analiptin, which can solve the problems of expensive hydroxybenzotriazole condensing agent, difficult industrial scale-up, harsh reaction conditions, etc., and achieves great practical application value, The effect of high overall yield and easy purification
Inactive Publication Date: 2015-10-14
CISEN PHARMA +1
View PDF3 Cites 1 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
[0015] Among them, method 1 is prepared by activating intermediate 2 with N-(3-dimethylaminopropyl)-N'-ethylcarbodiimide hydrochloride (ECDI) and hydroxybenzotriazole (HOBT) condensing agent Anagliptin, the hydroxybenzotriazole condensing agent used is more expensive, and it is difficult to realize industrial scale-up
Me...
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.
[0076] Suspend the compound of formula (1) (30g) and N-hydroxysuccinimide (19.5g) in 200mL of dichloromethane, add EDCI (36g) in dichloromethane mixture in batches under ice-cooling, and stir at room temperature after adding 8 hours. After filtration, 40 g of white solid O-2,5-dicarbonylpyrrolyl-2-methylpyrazolo[1,5-a]pyrimidine-6-carboxylate (5-1) was obtained, with a yield of 86%.
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 discloses a preparation method of anagliptin, which comprises the following steps: 1. activating a compound disclosed as Formula (2) to prepare a compound disclosed as Formula (5); and 2. condensing the compound disclosed as Formula (5) with a compound disclosed as Formula (3) or salts thereof to obtain the compound disclosed as Formula (1). The method has the advantages of cheap and accessible raw materials, mild reaction conditions, high reaction yield and easily purified intermediate, is simple to operate and suitable for industrial production, avoids the complex after-treatment processes, such as column chromatography, low-temperature reaction and the like, and greatly lowers the preparation cost. The intermediate (5) is subjected to condensation reaction and refined to obtain the anagliptin. The target product has the advantages of high purity and stable and controllable quality. The method overcomes the defects in the reported anagliptin preparation processes, and has great aggressive advancement effect and practical application value. Besides, the method is suitable for industrial production. The reaction general formula is disclosed in the specification.
Description
technical field [0001] The invention relates to a method for preparing antidiabetic medicine anagliptin. Background technique [0002] Anagliptin was developed by Sanwa Chemical Research Institute of Japan Co., Ltd. in November 2012, it was approved for marketing in Japan for the treatment of type II diabetes, and in December 2012 it was approved by the US FDA for the treatment of type II diabetes. Anagliptin is a dipeptidyl peptidase IV (DPP-IV) inhibitor, oral tablets one a day, good for the treatment and prevention of type II diabetes, and the treatment and prevention of complications of type II diabetes Effect. [0003] [0004] Anagliptin (1) [0005] 2-Methylpyrazolo[1,5-a]pyrimidine-6-carboxylic acid (2) is the key intermediate for the preparation of anagliptin, and its chemical structure is as follows: [0006] [0007] 2-Methylpyrazolo[1,5-a]pyrimidine-6-carboxylic acid (2) [0008] The original research patent WO2004067509 (same family patent CN100434420C...
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