CAS: 40805-79-6; 5-Pyrimidinecarbonitrile

相似化合物

10070-92-5 40929-49-5 4595-61-3

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CAS号40929-49-5 嘧啶-5-甲酰胺 | CAS号40929-50-8 嘧啶-5-甲酸乙酯 | CAS号90993-50-3 N-羟基-5-嘧啶羧酰胺

📜5-嘧啶甲酸乙酯置于ammonium Hydroxide,三乙胺,三氟乙酸酐体系中,用 二氯甲烷 作为反应溶剂,化学反应 16.0H,反应生成 5-氰基嘧啶
参考文献:恶二唑-异丙基酰胺作为有效的非共价蛋白酶体抑制剂
标题:恶二唑-异丙基酰胺作为有效的非共价蛋白酶体抑制剂
摘要:对 50 000 Chembridge 化合物库的筛选导致鉴定出恶二唑-异丙基酰胺1 (Pi-1833),其抑制胰凝乳蛋白酶样 (Ct-L) 活性(ic 50 = 0.60 μm),对其他两种主要蛋白酶体几乎没有影响蛋白水解活性,胰蛋白酶样 (Tl) 和谷氨酰肽水解样 (Pgph-L).lc-Ms/ms 和透析表明1是一种非共价且快速可逆的 Ct-L 抑制剂.集中文库合成为11Ad (Pi-1840) 提供了 Ct-L 活性 (Ic 50= 27 纳米).详细的 Sar 研究表明酰胺部分和两个苯环对修饰敏感.疏水性残基,如在对位丙基或丁基(未邻位或间位)的a环和一个的米-吡啶基团作为b环,显著提高活性.化合物11Ad (Ic 50 = 0.37 μm)在抑制完整 Mda-Mb-468 人乳腺癌细胞中的 Ct-L 活性和抑制其存活方面比1 (Ic 50 = 3.5 μm)更有效.11Ad的活
DOI:10.1021/jm400221D

专利信息

专利号:US-2003162992-A1
优先权日:2001-12-14
标 题 :Preparation of intermediates useful in the synthesis of antiviral nucleosides
发明人：WATANABE KYOICHI A; DU JINFA
摘要:The present invention is an efficient process for the manufacture of α-acyloxyacetaldehyde, a key intermediate in the synthesis of 1,3-oxathiolane and 1,3-dioxolane nucleosides.

专利号:EP-1501848-B1
优先权日:2002-05-08
标 题 :Synthesis of locked nucleic acid derivatives
发明人：SORENSEN MADS DETLEF; WENGEL JESPER; KOCH TROELS; CHRISTENSEN SIGNE M; ROSENBOHM CHRISTOPH; PEDERSEN DANIEL SEJER
权利人:SANTARIS PHARMA AS
摘要:The invention relates to a novel strategy for the synthesis of Locked Nucleic Acid derivatives, such as alpha-L-oxy-LNA, amino-LNA, alpha-L-amino-LNA, thio-LNA, alpha-L-thio-LNA, seleno-LNA and methylene LNA, which provides scalable high yielding reactions utilising intermediates that also can produce other LNA analogues such as oxy-LNA. Also, the compounds of the formula X are important intermediates that may be reacted with varieties of nucleophiles leading to a wide variety of LNA analogues. (Formula I)

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-2010204463-A1
优先权日:2007-08-07
标题 :Preparation Of Synthetic Nucleosides via Pi-Allyl Transition Metal Complex Formation
发明人：LIOTTA DENNIS C; LI YONGFENG
权利人:LIOTTA DENNIS C; LI YONGFENG
摘要:This invention provides highly regioselective and stereoselective processes for preparing synthetic nucleosides. A process for the preparation of synthetic nucleosides is provided that comprises a) preparing a bicycloamide derivative, b) reacting the bicycloamide derivative with a nucleic acid base or heterocyclic base or salt thereof in the presence of a transition metal catalyst to form a cyclopentenecarboxamide, and c) cleaving a carboxamide group from the cyclopentenecarboxamide to form the synthetic nucleoside. The processes according to the invention can be used for the synthesis of a variety of anti-viral agents, including Abacavir, Carbovir, and Entecavir, as well as derivatives thereof.

专利号:US-6927291-B2
优先权日:2001-03-01
标 题:Method for the synthesis of 2′,3′-dideoxy-2′,3′-didehydronucleosides
发明人：JIN FUQIANG; CONFALONE PASQUALE N
权利人:PHARMASSET LTD
摘要:An efficient synthetic route to antiviral 2′,3′-dideoxy-2′,3′-didehydro-nucleosides, such as 2′,3′-dideoxy and 2′- or 3′-deoxyribo-nucleoside analogs, from available precursors is disclosed, with the option of introducing functionality as needed. In one embodiment, a method for the preparation of β-D and β-L-2′,3′-dideoxy-2′,3′-didehydro-nucleosides is described that includes: activating a compound of structure (1) n n nwherein B is a pyrimidine or purine base and Y is O, S or CH 2 with an acyl halide of the formula X—C(â•?O)R 1 , X—C(â•?O)C(R 1 ) 2 OC(â•?O)R 1 or X—C(â•?O)OR 1 (wherein X is a halogen, and each R 1 is independently hydrogen, lower alkyl, alkyl, aryl or phenyl); reducing the resulting compound with a reducing agent to form a 2′,3′-dideoxy-2′,3′-didehydro-nucleoside; and optionally deprotecting the nucleoside. The haloacylation of the first step can form the 2′-acyl-3′-halonucleoside, the 3′-acyl-2′-halonucleoside, or a mixture thereof.

专利号:US-7595390-B2
优先权日:2003-04-28
标 题:Industrially scalable nucleoside synthesis
发明人：MOUSSA ADEL; WANG JING YANG; STORER RICHARD
权利人:NOVARTIS AG
摘要:An industrially scalable two-step process for preparing a β-L-2′-deoxy-nucleoside that results in a predominance of the β- over the α-anomeric form of the compound is described. An optional third step may be used to prepare 3′-prodrugs of desirable β-L-2′-deoxy-nucleosides for the delivery of these pharmaceuticals effective for treating viral diseases. The synthetic process is applicable in particular to the formation of β-L-2′-deoxy-cytidine, a pharmaceutically acceptable salt or prodrug thereof. The process can provide a relatively uncontaminated product that may require no further isolation or purification, thereby making the synthesis easily scalable for industrial manufacture.