CAS: 1809249-37-3; 2-Ethylbutyl ((S)-(((2R,3S,4R,5R)-5-(4-Aminopyrrolo[2,1-F][1,2,4]Triazin-7-yl)-5-Cyano-3,4-Dihydroxytetrahydrofuran-2-yl)Methoxy)(Phenoxy)Phosphoryl)-L-Alaninate

上下游产品

瑞德西韦杂质16 Remdesivir 1355050-11-1
瑞德西韦母核 Gs-441524 1191237-69-0
瑞德西韦5号中间体 (3Ar,4R,6R,6Ar)-4-(4-Aminopyrrolo[2,1-F][1,2,4]Triazin-7-yl)-6-(Hydroxymethyl)-2,2-Dimethyltetrahydrofuro[3,4-D][1,3]Dioxole-4-Carbonitrile 1191237-80-5
(3R,4R,5R)-2-(4-Aminopyrrolo[2,1-F][1,2,4]Triazin-7-yl)-3,4-Bis(Benzyloxy)-5-((Benzyloxy)Methyl)Tetrahydrofuran-2-Carbonitrile 1191237-68-9
瑞德西韦相关化合物5 (2R,3R,4R,5R)-2-(4-Aminopyrrolo[2,1-F][1,2,4]Triazin-7-yl)-3,4-Bis(Benzyloxy)-5-((Benzyloxy)Methyl)Tetrahydrofuran-2-Carbonitrile 1355357-49-1
瑞德西韦杂质1 (3R,4R,5R)-2-(4-Aminopyrrolo[2,1-F][1,2,4]Triazin-7-yl)-3,4-Bis(Benzyloxy)-5-((Benzyloxy)Methyl)Tetrahydrofuran-2-Ol 1355049-94-3
(2S,3R,4R,5R)-2-(4-Aminopyrrolo[2,1-F][1,2,4]Triazin-7-yl)-3,4-Bis(Benzyloxy)-5-((Benzyloxy)Methyl)Tetrahydrofuran-2-Ol

在 盐酸体系中,用 水,乙腈 用作溶剂,以47%的收率获得瑞德西韦
参考文献:一种瑞德西韦化合物的制备方法
标题:一种瑞德西韦化合物的制备方法
摘要:发明属于药物化学领域,具体涉及一种瑞德西韦化合物的新合成制备方法,以(2R,3R,4R,5R)‑2‑(4‑氨基吡咯[2,1‑f][1,2,4]三嗪‑7‑基)‑3,4‑二羟基‑5‑(羟基甲基)四氢呋喃‑2‑腈为起始原料,通过缩酮保护,Boc保护,拆分,磷酰化反应,取代反应,脱保护反应后制得瑞德西韦.本发明反应条件温和易控,操作简单,产品收率高,纯度高,适合工业化大生产.

专利信息

专利号:US-6683189-B1
优先权日:1996-02-26
标 题 :Method for the synthesis of pyrrole and imidazole carboxamides on a solid support
发明人：DERVAN PETER B; BAIRD ELDON
权利人:CALIFORNIA INST OF TECHN
摘要:The present invention describes a novel method for the solid phase synthesis of polyamides containing imidazole and pyrrole carboxamides. The polyamides are prepared on a solid support from aromatic carboxylic acids and aromatic amines with high stepwise coupling yields (>99%), providing milligram quantities of highly pure polyamides. The present invention also describes the synthesis of analogs of the natural products Netropsin and Distamycin A, two antiviral antibiotics. The present invention also describes a novel method for the solid phase synthesis of imidazole and pyrrole carboxamide polyamide-oligonucleotide conjugates. This methodology will greatly increase both the complexity and quantity of minor-groove binding polyamides and minor-groove binding polyamide-oligonucleotide conjugates which can be synthesized and tested.

专利号:US-10954178-B1
优先权日:2020-08-28
标题 :Synthesis of haloindenes
发明人：WNUK STANISLAW F; HOWLADER MD ABU HASAN
权利人:WNUK STANISLAW F; HOWLADER MD ABU HASAN; THE FLORIDA INTERNATIONAL UNIV BOARD OF TRUSTEES
摘要:The subject invention provides an expedited synthesis of 5, 6, and 7-iodoindenes from the corresponding aminoindan-1-ones in more than 70% yield, employing readily available precursors and reagents. A three-step sequence involves diazotization-iodination of aminoindan-1-one followed by reduction and dehydration. The method has a general character and can be extended for the preparation of various 4-, 5-, 6- or 7-haloindenes using different halogen sources for diazotization-halogenation reaction.

专利号:US-6639059-B1
优先权日:1999-03-24
标 题 :Synthesis of [2.2.1]bicyclo nucleosides
发明人：KOCHKINE ALEXEI; FENSHOLDT JEF; PFUNDHELLER HENRIK M
权利人:EXIQON AS
摘要:A synthesis of [2.2.1]bicyclo nucleosides which is shorter and provides higher overall yields proceeds via the key intermediate of the general formula III, wherein R4 and R5 are, for instance, sulfonates and R7 is, for instance, a halogen or an acetate. From compounds of the general formula II, such as 3-O-aryl-4-C-hydroxymethyl-1,2-O-isopropylidene-alpha-D-ribofuranose, intermediates of the general formula III are suitable for coupling with silylated nucleobases. Upon one-pot base-induced ring-closure and desulfonation of the formed [2.2.1]bicyclo nucleoside, a short route to each the LNA (Locked Nucleic Acid) derivatives of adenosine, cytosine, uridine, thymidine and guanidine is demonstrated. The use of the 5'-sulfonated ring-closed intermediate also allows for synthesis of 5'-amino- and thio-LNAs.

专利号:US-6734291-B2
优先权日:1999-03-24
标题:Synthesis of [2.2.1]bicyclo nucleosides
发明人：KOCHKINE ALEXEI; FENSHOLDT JEF; PFUNDHELLER HENRIK M
权利人:EXIQON AS
摘要:A synthesis of [2.2.1]bicyclo nucleosides which is shorter and provides higher overall yields proceeds via the key intermediate of the general formula III, wherein R4 and R5 are, for instance, sulfonates and R7 is, for instance, a halogen or an acetate. From compounds of the general formula II, such as 3-O-aryl-4-C-hydroxymethyl-1,2-O-isopropylidene-alpha-D-ribofuranose, intermediates of the general formula III are suitable for coupling with silylated nucleobases. Upon one-pot base-induced ring-closure and desulfonation of the formed [2.2.1]bicyclo nucleoside, a short route to each the LNA (Locked Nucleic Acid) derivatives of adenosine, cytosine, uridine, thymidine and guanidine is demonstrated. The use of the 5'-sulfonated ring-closed intermediate also allows for synthesis of 5'-amino- and thio-LNAs

专利号:WO-2024079704-A1
优先权日:2022-10-13
标题 :Synthesis of derivatives of siphonochilone and therapeutic use thereof
发明人：INVERNIZZI LUKE; MOYO PHANANKOSI; MAHARAJ VINESH
权利人:UNIV PRETORIA
摘要:THIS invention relates to the synthesis of derivatives of siphonochilone and therapeutic use thereof in the treatment and prevention of respiratory virus disease, in particular influenza or a coronavirus disease.

专利号:US-11655255-B2
优先权日:2022-10-17
标题 :Method for catalytic asymmetric synthesis of phosphorus-stereogenic (P-stereogenic) nucleoside derivative and catalyst used therein
发明人：ZHANG WANBIN; WANG MO; ZHANG LU; HUO XIAOHONG; ZHANG ZHENFENG; YUAN QIANJIA; CHEN JIANZHONG
权利人:SPH NO 1 BIOCHEMICAL & PHARMACEUTICAL CO LTD; UNIV SHANGHAI JIAOTONG
摘要:A method for catalytic asymmetric synthesis of a phosphorus-stereogenic (P-stereogenic) nucleoside derivative of formula (3) and a catalyst used therein. The P-stereogenic nucleoside derivative (3) can be hydrolyzed to obtain remdesivir. Specifically, a nucleoside and phosphoryl chloride are subjected to asymmetric reaction under the catalysis of a chiral bicyclic imidazole catalyst in the presence of a base to produce the P-stereogenic nucleoside derivative of formula (3)