Method for preparing fluoro alpha-D-arabinofuranose compound

A technology for furanoses and compounds is applied in the field of preparation of fluoro α-D-arabinofuranoses, and can solve the problems of many by-products, serious environmental pollution, difficulty in industrialized production and the like, and improve the reaction yield. , The effect of high product purity and convenient post-processing
CN101775044AActive Publication Date: 2010-07-14APELOA PHARM CO LTD +1
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
APELOA PHARM CO LTD
Publication Date
2010-07-14

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Abstract

The invention relates to a method for preparing a fluoro alpha-D-arabinofuranose compound. The method comprises the step of carrying out fluorination on substituted alpha-D-arabinofuranose compound (III) by an aryl sulfur fluoride fluoro reagent (II) so as to obtain a 2-deoxidized-2-fluorine substituted alpha-D-arabinofuranose compound (I). Compared with the traditional method, the preparation method has the advantages of simplicity, high product yield, less by-products, easy purification of products and high purity. The fluoro reagent causes less environmental pollution, is easy to store andtransport and is suitable for industrialized production. The reaction process is described in the specification of the invention.
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Description

technical field

[0001] The invention relates to a preparation method of fluorinated α-D-arabinofuranose compound. Background technique

[0002] Fluorinated α-D-arabinofuranose compounds, such as 2-deoxy-2-fluoro-1,3,5-tribenzoyl-α-D-arabinofuranose shown in formula (Ia), are the second An important intermediate of the purine nucleotide analogue clofarabine.

[0003] Take clofarabine whose structure is shown in formula (IV) as an example, it is a drug specially used for childhood leukemia, and is used as the main drug for treating refractory or relapsed acute lymphoblastic leukemia (ALL) aged 1-21, The cure rate of its treatment is high, the patient's tolerance is good, and there is no unpredictable adverse reaction.

[0004] Leukemia, especially acute lymphoblastic leukemia, is the most common malignancy in children and adolescents. Although the cure rate of childhood leukemia is relatively high, if it is treated with adult drugs, it will bring great toxic and side effect...

Claims

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