- Preparation method of cytarabine hydrochloride
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The invention provides a preparation method of cytarabine hydrochloride. The preparation method comprises following steps: A, cytidine and acetylsalicyl chloride are reacted so as to obtain acetyl cyclocytidine; B, acetyl cyclocytidine is subjected to deprotection in a hydrochloric acid methanol solution so as to obtain cyclocytidine hydrochloride; and C, cyclocytidine hydrochloride is subjected to ring-opening reaction so as to obtain cytarabine hydrochloride. The preparation method of cytarabine hydrochloride possesses following advantages: the raw materials are cheap and easily available; using of high toxicity substances difficult to remove is avoided; the preparation method is safe, and is friendly to the environment; and product yield and purity are high.
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Paragraph 0101-0103
(2019/03/28)
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- Process for producing 2,2'-o-cyclonucleosides nucleosides, and analogs thereof
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A novel process is provided for producing a nucleoside, such as cytarabine, or a nucleoside analogue, comprising the step of reacting 2,2'-O-cyclonucleoside or an analogue thereof with an amine. Preferably, the process is conducted in the presence of an aqueous solvent. A novel process for the production of the precursor 2,2'-O-cyclonucleoside compounds and pharmaceutically acceptable salts thereof is also provided which comprises reacting a 2,3'-O-diaikylstannylene nucleoside compound with an amine in the presence of a sulfonyl compound. Cytarabine is a known antineoplastic and antiviral agent.
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