- 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 0058-0061; 0070-0073; 0079-0082; 0088-0091
(2019/03/28)
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- PROTEIN BINDING COMPOUNDS
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The present invention provides a prodrug compound comprising a therapeutically effective moiety coupled via a metabolically cleavable bond to a blood protein binding moiety.
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Page/Page column 20-21
(2010/02/11)
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- Novel cytarabine monophosphate prodrugs
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Compounds of Formula I, their preparation and uses are described: wherein: M and V are cis to one another and MH is cytarabine; the 5′ oxygen of said cytarabine is attached to the phosphorus; V is 4-pyridyl; and pharmaceutically acceptable prodrugs and salts thereof.
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Page/Page column 22
(2008/06/13)
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- Method of treating nausea and vomiting with certain substituted-phenylalkylamino (and aminoacid) derivatives and other serotonin depleting agents
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A method for the treatment of emesis in a mammal, which method comprises administering to said mammal an emesis inhibiting amount of a compound which depletes serotonin in the brain of mammals; among which are compounds having the formula: STR1 wherein, R is selected from hydrogen, loweralkyl, trifluoromethyl, carboxyl, or loweralkoxycarbonyl; R1 and R2 are hydrogen or loweralkyl; Z is trifluoromethyl or halogen; the optical isomers and pharmaceutically acceptable salts thereof; two of the preferred compounds of the invention are fenfluramine and norfenfluramine.
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