Method for preparing 2', 3'2-dideoxycytidine

A technology of dideoxycytidine and its production method, which is applied in the field of anti-AIDS drugs and can solve problems such as low product yield and complex process

Inactive Publication Date: 2005-01-12
陆锦康
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] The existing production method of 2',3'-dideoxycytidine has complex process and low product yield

Method used

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  • Method for preparing 2', 3'2-dideoxycytidine
  • Method for preparing 2', 3'2-dideoxycytidine
  • Method for preparing 2', 3'2-dideoxycytidine

Examples

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Embodiment

[0020] A production method of 2', 3'-dideoxycytidine, comprising the following steps in sequence:

[0021] ①Reaction of cytidine and acetic anhydride to generate 4-N-acetyl cytidine: 10 grams of cytidine and 12-30ml (can be 12, 18, 25, 30ml) of acetic anhydride are heated under reflux for 10-20 Hours (Example 10, 15, 20 hours), then remove the solvent under reduced pressure, then add toluene 50×2 to azeotropically remove the residue to obtain a colorless powder product. Reaction formula:

[0022]

[0023] ②The 4-N-acetyl cytidine obtained above and the saturated acetic acid solution of hydrogen bromide are reacted under the condition of acetic anhydride as a catalyst to generate a brominated mixture, which is a pair of isomers: 10 grams of 4-N-acetyl Cytidine, add 5-15ml (Example 5, 10, 15ml) of saturated acetic acid solution of hydrogen bromide and 5-15ml (Example 5, 10, 15ml) of freshly distilled acetic anhydride, heat the oil bath to 40-60°C (Example 40, 50, 60°C), rea...

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Abstract

In this invention, cytidine reacts with acetic oxide to produce 4-N-acetylcytidine, then reacting with hydrogen bromide in acetic acid saturated solution, in the presence of acitic oxide as catalyst to produce bromo-mixture; then reacting in the presence of Zn-Cu couple as catalyst to produce 4-N-acetyl-2,3-dihydro-2,3-didioxy cytidine-5-acetate; then, reacting, to proceed hydrogenation reaction, in the presence of Pd/C, to produce 4-N-acetyl-2,3-dideoxy guanosine-5-acetate; then, reacting in the presence of methanol and triethylamine to produce 2,3-dideoxy cytidine. This invention has advantages of: simple process, easy to operate, available raw material, high yield over 90%.

Description

Technical field: [0001] The invention relates to a medicine, which is an anti-AIDS medicine. Background technique: [0002] The existing production method of 2',3'-dideoxycytidine has complex process and low product yield. Invention content: [0003] The purpose of the present invention is to provide a production method of 2',3'-dideoxycytidine with simple process, easy operation and high product yield. [0004] Technical solution of the present invention is: [0005] A method for producing 2', 3'-dideoxycytidine, characterized in that it comprises the following steps in sequence: [0006] ①Reaction of cytidine with acetic anhydride to generate 4-N-acetylcytidine; [0007] [0008] ②React 4-N-acetylcytidine and hydrogen bromide in a saturated acetic acid solution under the condition of acetic anhydride as a catalyst to generate a brominated mixture, which is a pair of isomers; [0009] [0010] ③React the above-mentioned brominated mixture under the condition of ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H19/073
Inventor 陆锦康王新华
Owner 陆锦康
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