CAS: 1532-84-9; Isoquinolin-1-Amine

相似化合物

25475-67-6 60448-38-6 19658-76-5

上下游产品

isoquinoline 1-nitro-isoquinoline isoquinoline1-(α-hydroxy-3,4-dimethoxybenzylidene)aminoisoquinoline toluene [1]isoquinolyl-picryl-amine N-(isoquinolin-1-yl)acetamide is°Chinolin2-Phenyl-imidazo2,1-ais°Chinolin (2,4-dinitro-phenyl)-[1]isoquinolyl-amine

异喹啉置于(Tmp)2Cu(Cn)Li2,O-苄基羟胺体系中,用 四氢呋喃 用作溶剂,化学反应 2.5H,以87%的收率获得1-氨基异喹啉
参考文献:通过去质子铜化作用直接羟基化和胺化芳烃
标题:通过去质子铜化作用直接羟基化和胺化芳烃
摘要:芳族/杂芳族 Ch 键的去质子定向邻铜化和随后用 T-Buooh 氧化以高产率和高区域选择性和化学选择性提供官能化酚.Dft 计算表明,这种羟基化反应通过铜 (I-> Iii-> I) 氧化还原机制进行的.将该反应应用于使用 Bnonh2 的芳族 Ch 胺化有效地提供了相应的伯苯胺.这些反应显示出广泛的范围和非常好的官能团兼容性.还展示了这些转化的催化版本.
Doi:10.1021/jacs.6B03855

专利信息

专利号:US-4514569-A
优先权日:1982-01-28
标 题 :Synthesis of 1-substituted isoquinolines
发明人：HENDRICKSON JAMES B; RODRIGUEZ CESAR
权利人:HENDRICKSON JAMES B; RODRIGUEZ CESAR
摘要:A method for the synthesis of particular isoquinoline compounds which are useful intermediates in the preparation of members of the family of opium alkaloids, such as morphine and codeine. Steps in the process include the acylation of the isoquinoline nitrogen; reaction of the acylated isoquinoline with a phosphorous compound; and condensation with a benzaldehyde derivative to yield a 1-benzyl isoquinoline.

专利号:US-4557866-A
优先权日:1984-05-15
标 题 :Process for the synthesis of pyrido-imidazo rifamycins
发明人：CANNATA VINCENZO; TAMAGNONE GIAN F
权利人:ALFA FARMACEUTICI SPA
摘要:A new process for the synthesis of pyrido-imidazo-rifamycins of formula I wherein R is hydrogen or acetyl, R1 and R2 independently represent hydrogen, (C1-4)-alkyl, benzyloxy, mono- or di-(C1-3)-alkylamino-(C1-4)-alkyl, (C1-3)-alkoxy-(C1-4)-alkyl, hydroxymethyl, hydroxy-(C2-4)-alkyl, cyano, halogen, nitro, mercapto, (C1-4)-alkylthio, phenylthio, carbamoyl, mono- or di-(C1-4)-alkyl-carbamoyl, or R1 and R2 taken together with two consecutive carbon atoms of the pyridine nucleus form a benzene ring optionally substituted by one or two methyl or ethyl groups. The process comprises reacting the rifamycin O of formula II with a 2-aminopyridine of formula III wherein R1 and R2 have the same meanings as before.

专利号:US-6340760-B1
优先权日:1998-06-26
标题:Process for the preparation of (S)-N-tert-butyl-1,2,3,4-tetrahydroisoquinoline-3-carboxyamide
发明人：BELLANI PIETRO; FRIGERIO MARCO
权利人:CLARIANT LSM ITALIA S P A
摘要:A description is given here of a novel process for the synthesis of N-carboxyanhydride of formula VIby reacting (3S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid with triphosgene in dioxane; a description is also given of a process for the synthesis of (S)-N-tert-butyl-1,2,3,4-tetrahydroisoquinoline-3-carboxyamide by treating the N-carboxyanhydride VI so obtained with tert-butylamine.

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-2011137038-A1
优先权日:2006-11-09
标题 :Synthesis of selected stereoisomers of certain substituted alcohols
发明人：HARMS ARTHUR E
权利人:HARMS ARTHUR E
摘要:A process for producing one selected stereoisomer of a substituted alcohol comprises reacting a stereoisomeric epoxide with an amine, a carboxylic acid, an amide, a sulfonyl, or a cyanide. The process avoids the production of a racemic mixture of stereoisomers of the prior art. Such a stereoisomeric substituted alcohol can be used for anti-inflammatory therapy.

专利号:US-3954771-A
优先权日:1972-06-16
标题 :Process for the preparation of 2H-3-isoquinolones
发明人：GEERTS JEAN-PIERRE JULES; LINZ RAYMOND ARMAND
权利人:UCB SA
摘要:A process for the preparation of 2H-3-isoquinolones having the formula ##SPC1## n Wherein R 1 and R 2 are each hydrogen, halogen, lower alkyl, lower alkoxy, aryl, haloaryl, alkylaryl or alkoxyaryl; R 3 and R 4 are each hydrogen, lower alkyl, lower alkoxyalkyl, lower alkenyl, lower alkynyl, cycloalkyl, aryl, aralkyl, or halo-aralkyl, which comprises cyclizing an N-formyl-2-phenyl-acetamide of the formula ##SPC2## n Wherein R 1 , R 2 , R 3 and R 4 have the same meaning as above, with a cyclodehydration agent. Said 2H-3-isoquinolones are useful as starting materials e.g. in the synthesis of 1,4-dihydro-1,4-etheno-isoquinolin-3(2H)-ones which are valuable chemotherapeutic agents in the treatment of disorders of the central nervous system, such as troubles of wakefulness, disorders of equilibrium and vertigo.