Process for the preparation of...

Organic compounds -- part of the class 532-570 series – Organic compounds – Nitrogen attached directly or indirectly to the purine ring...

Reexamination Certificate

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C544S314000

Reexamination Certificate

active

06274732

ABSTRACT:

FIELD OF THE INVENTION
The present invention relates to a process for the preparation of a compound of the general formula (I) and a novel reactant useful for the process.
The inventors have developed the compound of the formula (I) useful as an antivirus agent, especially for the treatment of AIDS (Korean patent application, No. 96-47458; PCT/KR96/00265).
In the above inventions, the compound of the formula (I) may be prepared by reacting a compound of the formula (II) with a compound of the formula (III). The reaction may be represented by the following scheme (1).
wherein Lie is a leaving group such as halogen atom, alkylsulfonyl, or arylsulfonyl.
The inventors have continued their efforts to improve the process for the preparation of the compound of the formula (I), and now found a novel reactant useful for the process. As the result, a simpler and more economic process for the preparation of the compound can be established by using the novel reactant.
SUMMARY OF THE INVENTION
Accordingly, an object of the invention is to provide a simple and economic process for the preparation of the compound of the formula (I).
Another object of the invention is to provide a new reactant which is useful for the process for the preparation of the compound of the formula (I).
DETAILED DESCRIPTION OF THE INVENTION
The process according to the present invention simplifies the synthesis and increases the yield of the objective compound, and may be represented by the following scheme (2).
wherein Lie is a leaving group such as halogen atom, alkylsulfonyl, or arylsulfonyl.
The compound of the formula (I) may be prepared by reacting a compound of the formula (IV) with a compound of the formula (III) in the presence of a base with injection of oxygen.
The bases used in the above reaction may include, for example, sodium bicarbonate, sodium carbonate, potassium carbonate and sodium hydride.
The solvents used in the reaction may include organic polar solvents such as dimethylformamide.
The catalysts such as lithium iodide, sodium iodide and potassium iodide may be used in the reaction.
The reaction may be carried out at the temperature of 10~100° C. for 4-72 hours.
Meanwhile, the new reacting compound of the formula (IV) of the invention may be prepared by the following reaction scheme (3).
The compound of the formula (IV) may be prepared by hydrolyzing a compound of the formula (V) in the presence of an acid.
The starting material of the formula (V) may be prepared by various known methods.
Acids used in the reaction may include, for example, hydrochloric acid and sulfuric acid.
The reaction may be carried out at the temperature of 25~120° C. for 1-48 hrs.


REFERENCES:
patent: 5922727 (1999-07-01), Cho et al.

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