CAS: 143157-22-6; ((2R,3R,5S)-3-(Benzoyloxy)-4,4-Difluoro-5-Hydroxytetrahydrofuran-2-yl)Methyl Benzoate

相似化合物

1173824-58-2 122111-01-7 97614-44-3

上下游产品

2-deoxy-2,2-difluoro-D-erythro-pentonic acid γ-lactone 3,5-dibenzoate benzoyl chloride 2-deoxy-2,2-difluoro-1-carbonylribose ethyl (3R,S)-2,2-difluoro-3-hydroxy-(2,2-dimethyldioxolpent-4-yl)propionate 1-(3,5-di-O-benzoyl-2-deoxy-2,2-difluoro-β-D-erythro-pentofuranos-1-yl)-5-iodouracil 1-(3,5-di-O-benzoyl-2-deoxy-2,2-difluoro-β-D-erythro-pentofuranos-1-yl)-5-bromouracil 1-(3,5-di-O-benzoyl-2-deoxy-2,2-difluoro-β-D-erythro-pentofuranos-1-yl)-5-chlorouracil 1-(3,5-di-O-benzoyl-2-deoxy-2,2-difluoro-β-D-erythro-pentofuranos-1-yl)thymine

2-脱氧-2,2-二氟戊呋喃糖-1-酮 3,5-二安息香酸盐置于potassium Tert-Butylate,Aluminum Isopropoxide体系中,用 异丙醇,甲苯 用作溶剂,化学反应 1.5H,反应生成2-脱氧-2,2-二氟-3,5-二苯甲酰基-D-呋喃核糖
参考文献:一种吉西他滨中间体甲磺酰酯的制备方法
标题:一种吉西他滨中间体甲磺酰酯的制备方法
摘要:本发明涉及一种吉西他滨中间体甲磺酰酯的制备方法,属于药物中间体合成技术领域.为了解决现有的方法转化率低和废液量大的问题,提供一种吉西他滨中间体甲磺酰酯的制备方法,该方法包括在非水溶性有机溶剂和催化量异丙醇混合的溶剂中,使式ⅰ化合物2‑脱氧‑2,2‑二氟‑d‑赤型‑1‑呋喃酮糖‑3,5‑二苯甲酰酯在异丙醇铝和叔丁醇钠的共同存在下进行还原反应转化为式ⅱ化合物;降温将反应液温度控制在5oc以下,加入甲基磺酰氯进行酯化反应,得到相应的式ⅲ化合物吉西他滨中间体甲磺酰酯.本发明能够有效的提高反应的速度和转化率,减少了杂质的产生,具有较高的收率和纯度要求,且能够实现一锅法反应,简化了生产操作.

专利信息

专利号:US-10751358-B2
优先权日:2017-04-26
标题 :Multitargeted nucleoside derivatives
发明人：KALMAN THOMAS I
权利人:KALMAN THOMAS I
摘要:Multitargeted pyrimidine nucleoside carbamates, substituted with fluorine at both the base and the sugar moieties, are disclosed (see Formula I): n nwhere R=linear or branched alkyl (C 1-7 ); R′=H, hydroxy protecting group; R″=H, phosphate ester, amino acid alkyl (C 1-7 ) ester phoshoramidate, or phosphorodiamidate. The disclosed compounds are fluoropyrimidine prodrugs that are characterized by a novel combination of structural components that provide intracellular metabolites capable of 1) inhibiting several cellular enzymes required for the synthesis and proper functioning of DNA, and 2) causing DNA damage by misincorporation into DNA. By acting on multiple targets with different mechanisms of action, compounds of Formula I reduce the likelihood of the emergence of drug resistance, a major drawback of the use of nucleoside-based anticancer and antiviral drugs. Due to the metabolic activation profile of compounds of Formula I, characteristic adverse effects and potential lethality of the fluoropyrimidine class of anticancer drugs may be alleviated. Compounds and compositions of the present disclosure can be used in treatment of cancer and viral infections.