Method for synthesizing entecavir

A technology of entecavir and a synthetic method, applied in directions such as organic chemistry, can solve problems such as high cost, low yield, complicated reaction, etc., and achieve the effects of low production cost, convenient operation and simple process

Inactive Publication Date: 2008-08-06
陆锦康
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At home and abroad, there are many patents and documents about its synthetic route, but there are generally defects such as difficult access to raw materials, high cost, low yield, and complex reactions.

Method used

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  • Method for synthesizing entecavir
  • Method for synthesizing entecavir
  • Method for synthesizing entecavir

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0029] 1. Preparation of Ente-0:

[0030] Ente-0 is prepared by reacting 2-amino-6-chloropurine with benzyl alcohol in the presence of NaH and 1,4-dioxane. The reaction formula is:

[0031]

[0032] Specific operation: In the reaction flask, add 400g NaH and 12L 1,4-dioxane, dropwise add 1040g benzyl alcohol, stir at room temperature for 1h (hour), add 800g 2-amino-6-chloropurine, and complete the addition , heat up to reflux, react for 48 hours, stop heating, add the reaction solution into 50L ice water, stir to precipitate solids, filter to remove solids, keep the filtrate at 10°C, adjust the pH of the filtrate to 6-7 with glacial acetic acid, precipitate solids, and filter , wash the filter cake with methanol, and dry the solid to obtain Ente-0.

[0033] 2. Preparation of Ente-2:

[0034] Reaction of Ente-1 and Ente-0 in the presence of LiH and DMF to prepare Ente-2, the reaction formula:

[0035]

[0036] Feeding:

[0037] Name Feeding

[0038] Ente-0 720g

[0...

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Abstract

The invention discloses a synthesis method of entecavir, which sequentially comprises the preparations of Ente-0, Ente-1, Ente-2, Ente-3, Ente-4, Ente-5 and Ente-6; and a process for producing product from Ente-6. The synthesis method of entecavir has easily obtained materials, simple process, low production cost and easy operation.

Description

Technical field: [0001] The invention relates to a production method of medicine. Background technique: [0002] Due to the rapid expansion of the health problems caused by virus infection, many institutions have invested a lot of research on antiviral drugs. Since 1995, 2 to 3 new antiviral varieties have been launched every year, which is the fastest-growing drug in the history of antiviral drug development. This is the culprit that endangers human health. [0003] Entecavir (2-amino-9-[(1S, 3R, 4S * )-4-hydroxy-3-hydroxymethyl-2-methylenecyclopentyl]-1,9-dihydro-6H-purin-6-one-hydrate entecavir) is a guanosine analog , and its molecular structure is: [0004] [0005] Entecavir [0006] Entecavir was first confirmed in HepG2.2.15 cells in 1997 that it has higher inhibitory activity on wild-type HBV virus than lamivudine. The FDA officially announced the approval of the market, becoming the third nucleoside drug for the treatment of hepatitis B...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D473/18
Inventor 陆锦康陆誉升杜永李建国
Owner 陆锦康
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