Adefovir (AD) monoester and preparation method thereof
A technology of adefovir dipivoxil and monoester, which is applied in the field of pharmaceutical chemical synthesis, can solve the problems of poor physical and chemical stability, lower oral bioavailability, and easy hydrolysis, etc., and achieve shortened production cycle, low production cost, and simple industrial equipment Effect
Active Publication Date: 2010-08-25
天津泰普制药有限公司 +1
View PDF3 Cites 1 Cited by
- Summary
- Abstract
- Description
- Claims
- Application Information
AI Technical Summary
Problems solved by technology
However, due to its poor physical and chemical stability, adefovir dipivoxil is prone to hydrolysis, and an esterification group is removed to generate adefovir monoplastil and adefovir, which changes the quality of the product and reduces the oral bioavailability
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 moreImage
Smart Image Click on the blue labels to locate them in the text.
Smart ImageViewing Examples
Examples
Experimental program
Comparison scheme
Effect test
Embodiment 1
Embodiment 2
Embodiment 3
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 Adefovir (AD) monoester and a preparation method thereof, wherein the Adefovir monoester uses Cu-Kalpha radiation, an X-ray powder diffraction spectrum expressed by using a 2theta degree has peaks at 3.60, 3.96, 6.00, 12.66, 13.20, 14.38, 15.40, 15.80, 16.26, 16.78, 17.84, 18.10, 18.60, 19.84, 20.74, 24.28, 24.56, 26.42 and 28.70, and the melting point is 188-192 DEG C. The preparation method comprises the following steps of: dissolving the AD into water or a mixed solvent of acetonitrile and water; stirring and heating to 30-60 DEG C; adding weak base to carry out a hydrolysis reaction; decompressing and concentrating after an HPLC (High Performance Liquid Chromatography) detection completely reacts; and treating to obtain a white monoester fine product. The prepared AD monoester has good quality, and the HPLC normalization method purity can reach higher than 99 percent.
Description
technical field The invention belongs to the technical field of pharmaceutical chemical synthesis, and relates to a synthetic method of 9-[2-[(pivaloyloxymethoxy)phosphorylmethoxy]ethyl]adenine (abbreviated as adefovir monoplastil). Specifically, it is adefovir monoester and its preparation method. Background technique Hepatitis B remains a global health threat. About 1.2 million people die from hepatitis B and related diseases every year, and chronic hepatitis B carriers account for 5% of the global population. Currently, there are two basic ways to treat chronic hepatitis B, one is immune activation therapy such as interferon, and the other is drugs that inhibit virus replication, such as adefovir dipivoxil, which is already on the market, and its trade name is Daiding. Adefovir dipivoxil is currently recognized as one of the first-line antiviral drugs for hepatitis B in the world. It has a wide range of antiviral effects, including hepatitis B virus (HBV), human immuno...
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
Login to View More IPC IPC(8): C07F9/6561
Inventor 董亚博赵健马克刘亚梅杨昕
Owner 天津泰普制药有限公司