CAS: 134877-42-2; ((2R,3R,5R)-3-(Benzoyloxy)-4,4-Difluoro-5-((Methylsulfonyl)Oxy)Tetrahydrofuran-2-yl)Methyl Benzoate

上下游产品

CAS号124-63-0 甲基磺酰氯 | CAS号1173824-58-2 2-脱氧-2,2-二氟-D-赤... | CAS号122111-01-7 2-脱氧-2,2-二氟戊呋喃糖... | CAS号143157-24-8 1'-表 2',2'-二氟-2... | CAS号143157-27-1 2',2'-二氟-2'-脱氧尿... | CAS号134790-40-2 1'-表吉西他滨3',5'-二苯甲酸酯 | CAS号134790-39-9 2'-脱氧-3',5'-二-O... | CAS号122111-05-1 4-Amino-1-(2-de... | CAS号122111-03-9 盐酸吉西他滨

2-脱氧-2,2-二氟-D-赤式-五呋喃糖-3,5-二苯甲酯-1-甲磺酸酯 以 乙醇 用作溶剂,以81%的收率获得2-脱氧-2,2-二氟-呋喃核糖基-3,5-二苯甲酰基-1-甲磺酸酯
参考文献:吉西他滨关键中间体磺化糖的工业制备工艺
标题:吉西他滨关键中间体磺化糖的工业制备工艺
摘要:本发明涉及式(i)化合物,即吉西他滨关键中间体磺化糖的制备方法,式(ⅱ)化合物经硼氢化钠还原,羟基保护,拆分得最终产物.该方法工艺简单,产率高,产品纯度好,无需苛刻的反应条件,十分适合工业生产.(i).

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.