CAS: 161599-46-8; (2R,3R,4R,5R)-2-(4-Amino-5-Fluoro-2-Oxopyrimidin-1(2H)-yl)-5-Methyltetrahydrofuran-3,4-Diyl Diacetate

上下游产品

CAS号2022-85-7 5-氟胞嘧啶 | CAS号27821-07-4 (2S,3R,4R,5R)-5... | CAS号37076-71-4 三-o-乙酰基-5-脱氧-d-呋喃核糖 | CAS号41108-04-7 5-fluoro-2-trim... | CAS号108-24-7 乙酸酐 | CAS号66335-38-4 5'-脱氧-5-氟胞嘧啶核苷 | CAS号880633-97-6 5'-deoxy-2',3'-... | CAS号66335-38-4 5'-脱氧-5-氟胞嘧啶核苷 | CAS号162204-20-8 5'-脱氧-5-氟-N-[(戊... | CAS号124012-42-6 加洛他滨 | CAS号162204-22-0 2’,3’-二-O-乙酰基-5... | CAS号154361-50-9 卡培他滨

卡培他滨杂质25置于盐酸,偶氮二甲酸二异丙酯,1-Ethylpiperidine Hypophosphite,硫酸,四氯化锡,碳酸氢钠,三乙胺,Sodium Iodide体系中,用 1,4-二氧六环,二氯甲烷,水,乙腈 用作溶剂,化学反应 41.5H,反应生成2',3'-二-O-乙酰基-5'-脱氧-5-氟-D-胞啶
参考文献:卡培他滨及其中间体的制备方法
标题:卡培他滨及其中间体的制备方法
摘要:本发明公开了一种新的卡培他滨的制备方法:以d-核糖为起始原料,经羟基保护,5-位对甲苯磺酰化,碘取代,次磷酸脱碘,乙酰化得关键中间体12,3-三-O-乙酰基-5-脱氧-β-D-呋喃核糖,再与5-氟胞嘧啶进行糖苷化,最后n-4位酰化,脱除保护得卡培他滨,本发明不需要使用金属催化剂参与反应,反应条件温和,且收率较高,经济有效,适于大规模的工业化生产.

专利信息

专利号:US-8975393-B2
优先权日:2012-01-13
标 题:Synthesis of 5-deoxy-5′-fluorocytidine compounds
发明人：LIN KO-CHUNG; CHIEN CHUNGSUN
权利人:PHARMAESSENTIA CORP
摘要:This invention relates to a process of synthesizing a β-nucleoside compound of formula (I): n nwherein R 1 is alkyl, aryl, cycloalkyl, heteroaryl, or heterocycloalkyl. The process includes reacting a compound of formula (II):n n nwith a compound of formula (III):n n nwherein R 1 is as defined above and X is chloride, bromide, iodide, methanesulfonate, triflate, p-toluenesulfonate, trifluoroacetate, 4-nitrophenoxy, or N-succinimidyloxy, in a solvent and in the presence of a base.

专利号:US-2013184451-A1
优先权日:2012-01-13
标 题:Novel synthesis of 5-deoxy-5'-fluorocytidine compounds

专利号:US-2021171564-A1
优先权日:2018-08-03
标 题 :Compositions and methods for the treatment of cancer
发明人：KANDULA MAHESH
权利人:CELLIX BIO PRIVATE LTD; CELLIX BIO PROVATE LTD
摘要:The compositions and compounds of formula I and formula II which includes nucleic acid synthesis inhibitor conjugates or its polymorphs, enantiomers, stereoisomers, solvates, and hydrates thereof. These conjugates may be formulated as pharmaceutical compositions. The pharmaceutical compositions may be formulated for oral administration, intravenous, solution, syrup, sachet, transdermal administration, or injection. Such compositions may be used to treatment of cancer or its associated complications.

专利号:CN-103204889-B
优先权日:2012-01-13
标题 :Synthesis method of 5-deoxy-5' -fluorocytidine compound