CAS: 607-32-9; 5-Nitroisoquinoline

上下游产品

CAS号119-65-3 异喹啉 | CAS号118798-90-6 N-(2-Cyanoethyl... | CAS号57554-78-6 5-nitro-2-oxido... | CAS号708-14-5 3-氧代-1,3-二氢-2-苯... | CAS号108-24-7 乙酸酐 | CAS号7664-93-9 硫酸 | CAS号7697-37-2 硝酸 | CAS号109571-88-2 6-phenylisoquin... | CAS号109571-87-1 5-Isoquinolinam... | CAS号109571-89-3 6,8-diphenyliso... | CAS号111493-33-5 4,5-dinitroisoq... | CAS号41959-45-9 5-硝基1,2,3,4-四氢异喹啉 | CAS号46492-08-4 苯并[g]异喹啉-5,10-二酮 | CAS号296776-08-4 6-chloro-7-[4-(... | CAS号27536-05-6 N-(1,2,3,4-Tetr... | CAS号27461-33-2 5-乙酰氨基异喹啉 | CAS号603-11-2 3-硝基邻苯二甲酸

异喹啉置于硫酸,硝酸体系中,化学反应 2.0H,以52%的收率获得产物5-硝基异喹啉
参考文献:含四氢异喹啉部分的脲衍生物的合成及作为小鼠镇痛药物的生物学评价
标题:含四氢异喹啉部分的脲衍生物的合成及作为小鼠镇痛药物的生物学评价
摘要:瞬时受体电位香草素 1 (Trpv1) 是一种配体门控非选择性阳离子通道,被认为是重要的疼痛整合因子.trpv1 的原型拮抗剂四氢异喹啉具有明显的治疗潜力.在这里,设计并合成了一系列四氢异喹啉的脲衍生物.初步生物学试验表明化合物i 1,I 2 和i 9 具有非常好的trpv1拮抗活性.在进一步的研究中,I 1 在不同的疼痛模型中表现出比阳性对照 Bctc 更好的镇痛活性.所有这些结果表明 I 1 可以被认为是进一步开发抗伤害药物的主要候选药物.
DOI:10.1002/ardp.201400455

专利信息

专利号:US-6500954-B1
优先权日:1998-06-22
标 题:Synthesis of 5- or 8-bromoisoquinoline derivatives
发明人：GOULIAEV ALEX HAAHR; HANSEN WILLIAM
权利人:NEUROSEARCH AS
摘要:The present invention is directed to a method of preparing bromoisoquinoline derivatives, in particular 5- or 8-bromoisoquinoline derivatives. Bromoisoquinoline derivatives, and in particular 5-bromoisoquinoline and 5-bromo-8-nitroisoquinoline derivatives, are key intermediates in the synthesis of pharmaceutical compounds.

专利号:US-11999749-B2
优先权日:2021-06-30
标题 :Synthesis of a bis-mesylate salt of 4-amino-N-(1-((3-chloro-2-fluorophenyl)amino)-6-methylisoquinolin-5-yl)thieno[3,2-d]pyrimidine-7-carboxamide and intermediates thereto
发明人：GOSSELIN FRANCIS; KOENIG STEFAN G; MERCADO-MARIN EDUARDO V; STUMPF ANDREAS; ZELL DANIEL; ZHANG HAIMING; BACHMANN STEPHAN; CARRERA DIANE E; DALZIEL MICHAEL E; GE YONGHUI; ZHANG JIE; BIGLER RAPHAEL; FINET LAURE ELIZABETH SIMONE; MONDIERE REGIS JEAN GEORGES; NAKAGAWA YUKI
权利人:GENENTECH INC; HOFFMANN LA ROCHE
摘要:A manufacturing process to a bis-mesylate salt 1b of the pan-RAF inhibitor 4-amino-n-(1-((3-chloro-2-fluorophenyl)amino)-6-methylisoquinolin-5-yl)thieno[3,2-d]pyrimidine-7-carboxamide. The process features a number of efficient key reactions, including a robust and scalable Pd-catalyzed carbonylation reaction to generate thienopyrimidine 2 and a highly chemoselective Pt/V/C-catalyzed nitro group reduction to access penultimate intermediate 7. The final amide coupling of 7 and 2 was accomplished by a mild and safe protocol employing N,N,N′,N′-tetramethylchloroformamidinium hexafluorophosphate (TCFH) as the coupling reagent, to produce a 1:1 adduct of the freebase and THF. The adduct afforded compound 1b with excellent yield, purity, and form stability on a multikilogram production scale after reaction with MsOH and recrystallization. The methods are able to produce a compound having upwards of 95% purity.

专利号:US-2025051351-A1
优先权日:2021-06-30
标题 :Synthesis of a bis-mesylate salt of 4-amino-n-(1-((3-chloro-2-fluorophenyl)amino)-6-methylisoquinolin-5-yl)thieno[3,2-d]pyrimidine-7-carboxamide and intermediates thereto

专利号:US-2023028651-A1
优先权日:2021-06-30
标题 :Synthesis of a bis-mesylate salt of 4-amino-n-(1-((3-chloro-2-fluorophenyl)amino)-6-methylisoquinolin-5-yl)thieno[3,2-d]pyrimidine-7-carboxamide and intermediates thereto

专利号:TW-202311265-A
优先权日:2021-06-30
标 题 :Synthesis of a bis-mesylate salt of 4-amino-n-(1-((3-chloro-2-fluorophenyl)amino)-6-methylisoquinolin-5-yl)thieno[3,2-d]pyrimidine-7-carboxamide and intermediates thereto

专利号:US-10125226-B2
优先权日:2013-06-05
标 题 :Scale-up process of bifunctionalized triblock copolymers with secondary and tertiary amines, with application in dewatering and desalting of heavy crude oils
发明人：FLORES SANDOVAL CESAR ANDRES; FLORES OROPEZA EUGENIO ALEJANDRO; LOPEZ ORTEGA ALFONSO; HERNANDEZ CORTEZ JOSE GONZALO; ESTRADA BUENDIA ARISTEO; CASTRO SOTELO LAURA VERONICA; REYES MARTINEZ REYNA; ALVAREZ RAMIREZ FERNANDO; ESTRADA MARTINEZ ARQUIMEDES; VAZQUEZ MORENO FLAVIO SALVADOR
权利人:MEXICANO INST PETROL
摘要:A chemical synthesis process is provided for the functionalization of monodispersed triblock copolymer (POEw-POPy-POEw) with secondary or tertiary amines at a semi-industrial level in glass reactors having a capacity between 1 L and 100 L. The process includes two stages where the first stage uses an alkylsulfonyl or arylsulfonyl chloride to obtain better leaving groups, and the second stage is the nucleophilic substitution with secondary or tertiary amines, to obtain the bifunctionalized triblock copolymers. The main advantage for this process is to reduce the quantity of unitary process done in each stage, the optimization of reaction times, and the stoichiometric relationships.