CAS: 15397-15-6; (2S,3R,4R,5R)-5-((Benzoyloxy)Methyl)-3-Methyltetrahydrofuran-2,3,4-Triyl Tribenzoate

相似化合物

22224-41-5 30361-17-2 16434-48-3

上下游产品

methylmagnesium bromide benzoyl chloride 1,3,5-tri-O-benzoyl-2-oxo-α-D-erythro-pentofuranose methyltrichlorotitanium 2'-methyl-adenosine 2′,3′,5′-tri-O-benzoyl-2′-C-methyluridine

2-C-甲基-D-核糖酸-1,4-内酯置于吡啶,Sodium Hydride,溶剂黄146,三乙胺体系中,用 二氯甲烷 用作溶剂,化学反应 8.0H,反应生成1,2,3,5-四苯甲酰氧基-2-C-甲基-Beta-D-呋喃核糖
参考文献:一种(2'r)-2'-脱氧-2'-氟-2'-甲基脲苷的合 成工艺
标题:一种(2'r)-2'-脱氧-2'-氟-2'-甲基脲苷的合 成工艺
摘要:本发明公开了一种(2'R)‑2'‑脱氧‑2'‑氟‑2'‑甲基脲苷的合成工艺,涉及医药合成技术领域,解决了现有工艺成本高,产品收率低的技术问题.本发明通过使用硼氢化钠或者硼氢化钾来还原核糖内酯,避免使用昂贵的还原试剂红铝或者三叔丁氧基氢化铝锂,大大降低了成本;利用n,O‑双(三甲基硅基)乙酰胺作为硅醚化试剂提高糖苷化反应的收率,产品收率可达85‑90%,远高于路线三中的58%,产品收率显著提高;通过保护5'位的羟基可避免关环反应中的副反应,同时使用常见的极性溶剂二甲基甲酰胺,在碳酸氢钠催化下产品收率可达87‑92%.本发明的合成工艺易于操作,工艺条件更容易控制,降低成本,适用于大批量生产.

专利信息

专利号:US-7582748-B2
优先权日:2003-03-20
标题:Methods of manufacture of 2′-deoxy-β-L-nucleosides
发明人：RABI JAIME A
权利人:MICROBIOL QUIMICA FARMACEUTICA
摘要:The present invention relates to the synthesis of 2′-deoxy-β-L-thymidine, 2′-deoxy-β-L-uridine and 2′-deoxy-β-L-cytidine, and their derivatives, such as the 3′-O-acyl or 3′,5′-O-diacyl prodrugs, including the 3′-O-L-aminoacyl and 3′,5′-O-L-diaminoacyl prodrugs, and particularly the 3′-O-L-valinyl and 3′,5′-O-L-divalinyl prodrugs.

专利号:US-6891036-B2
优先权日:2003-02-10
标题:Process for the preparation of ribofuranose derivatives
发明人：TAMERLANI GIANCARLO; SALSINI LIANA; LOMBARDI ILARIA; BARTALUCCI DEBORA; CIPOLLETTI GIOVANNI
权利人:INALCO SPA
摘要:The present invention relates to a new process in 3 steps starting from 2-C-methyl-D-ribopentono-1,4-lactone for the preparation of tetra-acyl ribofuranose derivatives of formula (I): n n nuseful in the synthesis of nucleotides.

专利号:WO-2013066991-A1
优先权日:2011-10-31
标题 :Crystalline solvates of nucleoside phosphoroamidates, their stereoselective preparation, novel intermediates thereof, and their use in the treatment of viral disease
发明人：CHAMBERLAIN STANLEY; IGO DAVID; BIS JOANNA; SUKUMAR SENTHIL KUMAR KUSALAKUMARI
权利人:INHIBITEX INC
摘要:This invention is directed to novel crystalline solvates of the ( S )-P diastereomer of the anti- HCV nucleoside phosphoroamidate, (2 S )-neopentyl 2-((((2 R ,3 R ,4 R ,5 R )-5-(2-amino-6- methoxy-9H-purin-9-yl)-3,4-dihydroxy-4-methyltetrahydrofuran-2-yl)methoxy)(naphthalen- l-yloxy)phosphorylamino)propanoate (also referred to as INX-08189 or IÎ?Χ-189), and to a recrystallization method for separating the two diastereomers of INX-08189. In addition, this application relates to a novel stereoselective method for the preparation of either of the two diastereomers, and to the novel synthetic intermediates used in this stereoselective synthesis. The invention also relates to the use of the crystalline solvates to increase the liver exposure of 2'-C-methyl guanosine triphosphate from an oral dose.

专利号:US-9351989-B2
优先权日:2010-12-29
标 题:Substituted purine nucleosides, phosphoroamidate and phosphorodiamidate derivatives for treatment of viral infections
发明人：MCGUIGAN CHRIS; MADELA KAROLINA; BOURDIN CLAIRE; VERNACHIO JOHN; CHAMBERLAIN STANLEY
权利人:MCGUIGAN CHRIS; MADELA KAROLINA; BOURDIN CLAIRE; VERNACHIO JOHN; CHAMBERLAIN STANLEY; INHIBITEX INC; UNIV CARDIFF
摘要:This invention is directed to phosphoroamidate and phosphorodiamidate derivatives including the compounds of formula (I) having the structure n nwherein U, V, W, Z, R 1 , X 1 , X 2 , and Y are defined herein. These compounds and pharmaceutical compositions containing these compounds are useful in the treatment of viral infections in mammals infected by a virus in the Flaviviridae family of viruses, in particular hepatitis C virus (HCV). The compounds of this invention may be prepared by various methods known in the art of organic chemistry in general and nucleoside and nucleotide analog synthesis in particular.