Refining method of ganciclovir

A technology of ganciclovir and refining method, which is applied in the field of chemical refining, can solve the problems of reducing the impurity content of monocloganciclovir, etc., and achieve the effects of short refining period, high yield and low energy consumption

Active Publication Date: 2012-08-22
LIVZON GROUP CHANGZHOU KONY PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The synthetic method of ganciclovir mainly contains following two kinds: 1. diacetylguanine (or monoacetylguanine, or the mixture of monoacetylguanine and diacetylguanine) and 1,3-dihalo-2-( Acetoxymethoxy)propane carries out condensation reaction, then carries out displacement reaction with acetate to obtain triacetyl ganciclovir, then obtains ganciclovir through hydrolysis reaction; ② acetylguanine (or monoacetylguanine, Or the mixture of monoacetylguanine and diacetylguanine) and 1,3-diacetoxy-2-(acetoxymethoxy) propane) carry out condensation reaction to prepare triacetyl ganciclovir, then through Hydrolysis reaction to obtain ganciclovir, according to the above method ① and ② to prepare ganciclovir, the product will contain monocloganciclovir impurities, its structural formula is as follows, how to reduce the monocloganciclovir in ganciclovir The impurity content is rarely reported

Method used

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  • Refining method of ganciclovir

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] Put 30 g of crude ganciclovir with a monocloganciclovir content of 0.27%, 180 ml of water and 180 ml of DMF into a reaction flask, stir and heat to 93°C to dissolve, slowly cool to 70-80°C, keep stirring for 1 hour, and then Slowly cool to 40-50°C, stir for 1 hour, then cool to 20-30°C, stir for 2 hours, filter with suction, wash the filter cake with an appropriate amount of water, dry the crystallized product, and obtain 26.7g of ganciclovir fine product, single Chlorine impurity 0.048%.

Embodiment 2

[0016] Put 30g of crude ganciclovir with a monocloganciclovir content of 0.27%, 150ml of water and 210ml of DMF into the reaction bottle, stir and heat to dissolve at 100°C, slowly cool to 70-80°C, keep stirring for 1 hour, and then slowly Cool to 40-50°C, stir for 1 hour, then cool to 20-30°C, stir for 2 hours, filter with suction, wash the filter cake with an appropriate amount of water, take the crystallized product and dry to obtain 27.0g of ganciclovir fine product, monochlorinated Impurities 0.08%.

Embodiment 3

[0018] Put 30g of crude ganciclovir with a monocloganciclovir content of 0.27%, 300ml of water and 300ml of DMF into the reaction bottle, stir and heat to dissolve, slowly cool to 70-80°C, keep stirring for 1 hour, and then slowly cool to 40-50°C, stirred for 1 hour, then cooled to 20-30°C, stirred for 2 hours, filtered with suction, soaked in an appropriate amount of water to wash the filter cake, dried the crystallized product, and obtained 25.9 g of ganciclovir fine product, monoclonal impurity 0.04%.

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Abstract

The invention relates to the technical field of chemical refining, particularly a refining method of ganciclovir, which comprises the following steps: heating to dissolve a ganciclovir crude product in a water and DMF (N,N-dimethylformamide) mixed solution, cooling to crystallize in a gradient cooling mode, and filtering the crystallized product to obtain the ganciclovir. The method for lowering the monochloro-ganciclovir impurity content in ganciclovir can lower the monochloro-ganciclovir impurity content to less than 0.10%; and the invention has the advantages of short refinement period, low energy consumption and high yield, and is suitable for large-scale industrial production.

Description

technical field [0001] The invention relates to the technical field of chemical refining, in particular to a refining method of ganciclovir. Background technique [0002] The chemical name of ganciclovir is 9-(1,3-dihydroxy-2-propoxymethyl)-guanine, which is a nucleoside antiviral drug that can competitively inhibit DNA polymerase and incorporate into viruses and host cells DNA, inhibits DNA synthesis. Ganciclovir is a derivative of acyclovir, which is more effective than acyclovir, has a wider antiviral spectrum, has a highly specific effect on cytomegalovirus, and has a stronger inhibitory effect on human cytomegalovirus than acyclovir It has a certain effect on herpes simplex virus type I and type II, varicella zoster virus, Epstein-Barr virus, etc. This product was launched by Syntex Company of the United States and was approved for marketing in 1988. It is the first choice drug for the treatment of cytomegalovirus infection. [0003] The synthetic method of ganciclovi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D473/18
Inventor 陈敖俞军陈争一李鸣海
Owner LIVZON GROUP CHANGZHOU KONY PHARMA
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