394-67-2

Basic information

• Product Name: 4-Fluoroisoquinoline
• Synonyms: 4-fluoroisoquinoline sulfate;Isoquinoline, 4-fluoro-
• CAS NO: 394-67-2
• Molecular Formula: C₉H₆FN
• Molecular Weight: 147.15
• Mol File: 394-67-2.mol
• Article Data: 13

Chemical Properties

• Melting Point: 34 °C
• Boiling Point: 240℃
• Flash Point: 99℃
• Appearance: /
• Density: 1.216
• Vapor Pressure: 0.061mmHg at 25°C
• Refractive Index: 1.5914
• Storage Temp.: 2-8°C
• PKA: 3.45±0.10(Predicted)
• CAS DataBase Reference: 4-Fluoroisoquinoline(CAS DataBase Reference)
• NIST Chemistry Reference: 4-Fluoroisoquinoline(394-67-2)
• EPA Substance Registry System: 4-Fluoroisoquinoline(394-67-2)

Safety Data

• Hazardous Substances Data: 394-67-2(Hazardous Substances Data)

Usage

Uses

4-fluoroisoquinoline is a useful research chemical.

InChI:InChI=1/C9H6FN/c10-9-6-11-5-7-3-1-2-4-8(7)9/h1-6H

Synthetic route

4-bromoisoquinoline (1532-97-4) → 4-­fluoroisoquinoline (394-67-2)

Conditions	Yield
With potassium fluoride; C114H158O4P2Pd2; silver fluoride In tert-butyl methyl ether at 110℃; for 14h; Sealed tube;	90%
Stage #1: 4-bromoisoquinoline With n-butyllithium In tetrahydrofuran at -65℃; for 0.5h; Stage #2: With N-fluorobis(benzenesulfon)imide In tetrahydrofuran at -65℃; for 2h;	60%
Stage #1: 4-bromoisoquinoline With n-butyllithium In tetrahydrofuran; hexane at -65℃; for 1.5h; Cooling with acetone-dry ice; Stage #2: With N-fluorobis(benzenesulfon)imide In tetrahydrofuran; hexane at -65℃; for 1h;
Stage #1: 4-bromoisoquinoline With n-butyllithium In tetrahydrofuran; hexane at -65℃; for 1.5h; Stage #2: With N-fluorobis(benzenesulfon)imide In tetrahydrofuran; hexane at -65℃; for 2h; Stage #3: With sodium hydrogencarbonate In water; ethyl acetate at 20℃; for 12h;
Stage #1: 4-bromoisoquinoline With n-butyllithium In tetrahydrofuran; hexane at -65℃; for 1.5h; Stage #2: With N-fluorobis(benzenesulfon)imide In tetrahydrofuran; hexane at -65 - 20℃;

4-aminoisoquinoline (23687-25-4) → 4-­fluoroisoquinoline (394-67-2)

Conditions	Yield
Stage #1: 4-aminoisoquinoline With lithium tetrafluoroborate; tert.-butylnitrite; trifluoroacetic acid In ethyl acetate at 60℃; Balz-Schiemann Reaction; Flow reactor; Stage #2: With lithium tetrafluoroborate In ethyl acetate Flow reactor;	74%
Stage #1: 4-aminoisoquinoline With tetrafluoroboric acid; sodium nitrite In water at -10 - -8℃; for 1h; Stage #2: In toluene at 90℃; for 1h;	8%

isoquinoline-4-diazonium-tetrafluoroborate → 4-­fluoroisoquinoline (394-67-2)

4-bromoisoquinoline (1532-97-4) + N-fluorobis(benzenesulfon)imide (133745-75-2) → 4-­fluoroisoquinoline (394-67-2)

Conditions	Yield
Stage #1: 4-bromoisoquinoline With n-butyllithium In tetrahydrofuran at -65℃; for 0.5h; Stage #2: N-fluorobis(benzenesulfon)imide In tetrahydrofuran at -65 - 25℃; for 11.5h; Inert atmosphere;

1-isoquinolone (491-30-5) → isoquinoline (119-65-3) + 4-­fluoroisoquinoline (394-67-2)

Conditions	Yield
Multi-step reaction with 3 steps 1.1: Selectfluor / acetonitrile / 2.5 h / 20 °C / Inert atmosphere 2.1: trichlorophosphate / dichloromethane / 20 - 47 °C 2.2: 2 h / 65 - 67 °C 3.1: palladium 10% on activated carbon; hydrogen / ethanol / 20 °C / 760.05 Torr View Scheme
Multi-step reaction with 3 steps 1: Selectfluor / acetonitrile / 2.5 h / 20 °C / Inert atmosphere 2: trichlorophosphate / dichloromethane / 20 - 47 °C 3: palladium 10% on activated carbon; hydrogen / ethanol / 20 °C / 760.05 Torr View Scheme
Multi-step reaction with 4 steps 1: Selectfluor / acetonitrile / 2.5 h / 20 °C / Inert atmosphere 2: trichlorophosphate / dichloromethane / 20 - 47 °C 3: trichlorophosphate / 2.5 h / 66 - 68 °C 4: palladium 10% on activated carbon; hydrogen / ethanol / 20 °C / 760.05 Torr View Scheme
Multi-step reaction with 4 steps 1: Selectfluor / acetonitrile / 2.5 h / 20 °C / Inert atmosphere 2: hydrogenchloride / dichloromethane; ethyl acetate / 6 h / 20 °C 3: trichlorophosphate / 2.5 h / 66 - 68 °C 4: palladium 10% on activated carbon; hydrogen / ethanol / 20 °C / 760.05 Torr View Scheme

C10H10FNO2 → isoquinoline (119-65-3) + 4-­fluoroisoquinoline (394-67-2)

Conditions	Yield
Multi-step reaction with 2 steps 1: trichlorophosphate / dichloromethane / 20 - 47 °C 2: palladium 10% on activated carbon; hydrogen / ethanol / 20 °C / 760.05 Torr View Scheme
Multi-step reaction with 3 steps 1: trichlorophosphate / dichloromethane / 20 - 47 °C 2: trichlorophosphate / 2.5 h / 66 - 68 °C 3: palladium 10% on activated carbon; hydrogen / ethanol / 20 °C / 760.05 Torr View Scheme
Multi-step reaction with 3 steps 1: hydrogenchloride / dichloromethane; ethyl acetate / 6 h / 20 °C 2: trichlorophosphate / 2.5 h / 66 - 68 °C 3: palladium 10% on activated carbon; hydrogen / ethanol / 20 °C / 760.05 Torr View Scheme

4-fluoroisoquinolin-1(2H)-one → isoquinoline (119-65-3) + 4-­fluoroisoquinoline (394-67-2)

Conditions	Yield
Multi-step reaction with 2 steps 1: trichlorophosphate / 2.5 h / 66 - 68 °C 2: palladium 10% on activated carbon; hydrogen / ethanol / 20 °C / 760.05 Torr View Scheme

1-chloro-4-fluoroisoquinoline → isoquinoline (119-65-3) + 4-­fluoroisoquinoline (394-67-2)

Conditions	Yield
With palladium 10% on activated carbon; hydrogen In ethanol at 20℃; under 760.051 Torr; Reagent/catalyst; Overall yield = 33 mg;

1-hydroxyisoquinoline (491-30-5) → 4-­fluoroisoquinoline (394-67-2)

Conditions	Yield
Multi-step reaction with 4 steps 1: Selectfluor / acetonitrile; methanol / 3 h / Reflux 2: hydrogenchloride / water; ethyl acetate 3: trichlorophosphate / 3 h / Reflux 4: palladium on activated charcoal; sodium hydroxide; hydrogen / methanol; water / 3 h / 20 °C View Scheme

4-fluoro-3-methoxyisoquinolin-1-ol → 4-­fluoroisoquinoline (394-67-2)

Conditions	Yield
Multi-step reaction with 3 steps 1: hydrogenchloride / water; ethyl acetate 2: trichlorophosphate / 3 h / Reflux 3: palladium on activated charcoal; sodium hydroxide; hydrogen / methanol; water / 3 h / 20 °C View Scheme

4-fluoroisoquinolin-1-ol → 4-­fluoroisoquinoline (394-67-2)

Conditions	Yield
Multi-step reaction with 2 steps 1: trichlorophosphate / 3 h / Reflux 2: palladium on activated charcoal; sodium hydroxide; hydrogen / methanol; water / 3 h / 20 °C View Scheme

1-chloro-4-fluoroisoquinoline → 4-­fluoroisoquinoline (394-67-2)

Conditions	Yield
With palladium on activated charcoal; hydrogen; sodium hydroxide In methanol; water at 20℃; for 3h;

1-bromoisoquinoline (1532-71-4) → 4-­fluoroisoquinoline (394-67-2)

Conditions	Yield
Multi-step reaction with 2 steps 1: N-fluorobis(benzenesulfon)imide / acetonitrile / 6 h / 60 °C 2: hydrogen / water; methanol / 6 h / 20 °C / Flow reactor; Alkaline conditions View Scheme

1-­bromo-4-fluoroisoquinoline (1421517-86-3) → 4-­fluoroisoquinoline (394-67-2)

Conditions	Yield
With hydrogen In methanol; water at 20℃; for 6h; Temperature; Flow reactor; Alkaline conditions;

4-­fluoroisoquinoline (394-67-2) → 4-fluoroisoquinoline sulfate (906820-09-5)

Conditions	Yield
With sulfuric acid In acetone at 0 - 10℃; for 2h; Inert atmosphere; Large scale reaction;	99%
With sulfuric acid In acetone at 0 - 10℃; for 2h;	98.8%
With sulfuric acid In acetone at -5℃; for 2h; Temperature;

4-­fluoroisoquinoline (394-67-2) → 4­-fluoroisoquinoline N­-oxide (1008-32-8)

Conditions	Yield
With 3-chloro-benzenecarboperoxoic acid In dichloromethane at 0 - 20℃; for 14h;	88%

4-­fluoroisoquinoline (394-67-2) + 1-phenylcyclopropan-1-ol (29526-96-3) → 3-(4-fluoroisoquinolin-1-yl)-1-phenylpropan-1-one

Conditions	Yield
With dipotassium peroxodisulfate In water; dimethyl sulfoxide at 70℃; for 12h; Inert atmosphere;	68%

2-methyltetrahydrofuran (96-47-9) + 4-­fluoroisoquinoline (394-67-2) → 4-fluoro-1-(5-methyltetrahydrofuran-2-yl)isoquinoline

Conditions	Yield
With C24H42N3(1+)*ClO4(1-); lithium perchlorate; acetic acid; trifluoroacetic acid In acetonitrile at 20℃; for 36h; Irradiation; Electrochemical reaction; Inert atmosphere; regioselective reaction;	61%

4-­fluoroisoquinoline (394-67-2) → C9H5ClFNO2S*ClH (1334294-10-8) + 4-fluoroisoquinoline-5-sulfonyl chloride hydrochloride (906820-08-4)

Conditions	Yield
Stage #1: 4-­fluoroisoquinoline With sulfuric acid at 10 - 40℃; for 0.5h; Stage #2: With sulfur trioxide at 20 - 45℃; for 12h; Stage #3: With hydrogenchloride; thionyl chloride; sodium hydrogencarbonate Product distribution / selectivity; more than 3 stages;	A n/a B 55%
With chlorosulfonic acid Inert atmosphere;	A 24 %Chromat. B 13 %Chromat.
Multi-step reaction with 2 steps 1.1: sulfuric acid / acetone / 2 h / 0 - 10 °C / Inert atmosphere; Large scale reaction 2.1: sulfur trioxide / ethyl acetate / 19 h / 30 °C / Inert atmosphere; Large scale reaction 2.2: 7 h / 30 - 70 °C / Inert atmosphere 2.3: 1 h / 35 °C / Inert atmosphere View Scheme

4-­fluoroisoquinoline (394-67-2) + 1-iodocyclohexane (626-62-0) → 1-cyclohexyl-4-fluoroisoquinoline

Conditions	Yield
With tert-butyl peroxyacetate; [4,4′-bis(1,1-dimethylethyl)-2,2′-bipyridine-N1,N1′]bis{3,5-difluoro-2-[5-(trifluoromethyl)-2-pyridinyl-κN]phenyl-κC}iridium(III) hexafluorophosphate; trifluoroacetic acid In acetonitrile at 20℃; for 24h; Inert atmosphere; Sealed tube; Irradiation;	49%

4-­fluoroisoquinoline (394-67-2) + 1,3-dioxoisoindolin-2-yl cyclohexanecarboxylate → 1-cyclohexyl-4-fluoroisoquinoline

Conditions	Yield
With tetrakis(acetonitrile)copper(I)tetrafluoroborate; 2.9-dimethyl-1,10-phenanthroline; zinc trifluoromethanesulfonate; 4,5-bis(diphenylphosphino)-9,9-dimethylxanthene In N,N-dimethyl acetamide for 24h; Inert atmosphere; Irradiation;	18%

4-­fluoroisoquinoline (394-67-2) → 4-fluoro-5-nitroisoquinoline (928664-13-5)

Conditions	Yield
Stage #1: 4-­fluoroisoquinoline With sulfuric acid; potassium nitrate at -5 - 5℃; for 1h; Stage #2: With ammonia In water pH=8;
With sulfuric acid; potassium nitrate In water at -5 - 0℃; for 1h;
Stage #1: 4-­fluoroisoquinoline With sulfuric acid; potassium nitrate at -5 - 5℃; Stage #2: With ammonia In water pH=8; Cooling with ice;
With sulfuric acid; nitric acid at 0 - 20℃; for 3h;	23 g
With sulfuric acid; potassium nitrate at 25℃; for 12h; Inert atmosphere;	5 g

4-­fluoroisoquinoline (394-67-2) → (S)-(-)-4-fluoro-N-(1-hydroxypropan-2-yl)isoquinoline-5-sulfonamide (223644-12-0)

Conditions	Yield
Multi-step reaction with 3 steps 1.1: sulfuric acid / acetone / 2 h / 0 - 10 °C / Inert atmosphere; Large scale reaction 2.1: sulfur trioxide / ethyl acetate / 19 h / 30 °C / Inert atmosphere; Large scale reaction 2.2: 7 h / 30 - 70 °C / Inert atmosphere 2.3: 1 h / 35 °C / Inert atmosphere 3.1: triethylamine / dichloromethane / -10 - 20 °C / Inert atmosphere; Large scale reaction View Scheme
Multi-step reaction with 2 steps 1: chlorosulfonic acid / Inert atmosphere 2: triethylamine / dichloromethane / -10 - 20 °C / Inert atmosphere; Large scale reaction View Scheme

4-­fluoroisoquinoline (394-67-2) → C12H11FN2O2S + C13H15FN2O5S2

Conditions	Yield
Multi-step reaction with 4 steps 1.1: sulfuric acid / acetone / 2 h / 0 - 10 °C / Inert atmosphere; Large scale reaction 2.1: sulfur trioxide / ethyl acetate / 19 h / 30 °C / Inert atmosphere; Large scale reaction 2.2: 7 h / 30 - 70 °C / Inert atmosphere 2.3: 1 h / 35 °C / Inert atmosphere 3.1: triethylamine / dichloromethane / -10 - 20 °C / Inert atmosphere; Large scale reaction 4.1: triethylamine / tetrahydrofuran / -10 - 0 °C / Inert atmosphere; Large scale reaction View Scheme
Multi-step reaction with 3 steps 1: chlorosulfonic acid / Inert atmosphere 2: triethylamine / dichloromethane / -10 - 20 °C / Inert atmosphere; Large scale reaction 3: triethylamine / tetrahydrofuran / -10 - 0 °C / Inert atmosphere; Large scale reaction View Scheme

4-­fluoroisoquinoline (394-67-2) → (S)-4-fluoro-N-[1-(3-hydroxypropylamino)propan-2-yl]isoquinoline-5-sulfonamide oxalate

Conditions	Yield
Multi-step reaction with 4 steps 1.1: sulfuric acid / acetone / 2 h / 0 - 10 °C / Inert atmosphere; Large scale reaction 2.1: sulfur trioxide / ethyl acetate / 19 h / 30 °C / Inert atmosphere; Large scale reaction 2.2: 7 h / 30 - 70 °C / Inert atmosphere 2.3: 1 h / 35 °C / Inert atmosphere 3.1: triethylamine / dichloromethane / -10 - 20 °C / Inert atmosphere; Large scale reaction 4.1: methanesulfonyl chloride; triethylamine / tetrahydrofuran / 20 h / -10 - 0 °C / Inert atmosphere; Large scale reaction 4.2: 0 - 25 °C / Inert atmosphere; Large scale reaction 4.3: 0.58 h / 75 °C / Inert atmosphere; Large scale reaction View Scheme
Multi-step reaction with 3 steps 1.1: chlorosulfonic acid / Inert atmosphere 2.1: triethylamine / dichloromethane / -10 - 20 °C / Inert atmosphere; Large scale reaction 3.1: methanesulfonyl chloride; triethylamine / tetrahydrofuran / 20 h / -10 - 0 °C / Inert atmosphere; Large scale reaction 3.2: 0 - 25 °C / Inert atmosphere; Large scale reaction 3.3: 0.58 h / 75 °C / Inert atmosphere; Large scale reaction View Scheme

4-­fluoroisoquinoline (394-67-2) → 4-fluoro-5-[[(2S)-hexahydro-2-methyl-1H-1,4-diazepin-1-yl]sulfonyl]isoquinoline hydrochloride (223644-02-8)

Conditions	Yield
Multi-step reaction with 5 steps 1.1: sulfuric acid / acetone / 2 h / 0 - 10 °C / Inert atmosphere; Large scale reaction 2.1: sulfur trioxide / ethyl acetate / 19 h / 30 °C / Inert atmosphere; Large scale reaction 2.2: 7 h / 30 - 70 °C / Inert atmosphere 2.3: 1 h / 35 °C / Inert atmosphere 3.1: triethylamine / dichloromethane / -10 - 20 °C / Inert atmosphere; Large scale reaction 4.1: methanesulfonyl chloride; triethylamine / tetrahydrofuran / 20 h / -10 - 0 °C / Inert atmosphere; Large scale reaction 4.2: 0 - 25 °C / Inert atmosphere; Large scale reaction 4.3: 0.58 h / 75 °C / Inert atmosphere; Large scale reaction 5.1: potassium carbonate / dichloromethane; water / 1 h / 20 °C / Inert atmosphere; Large scale reaction 5.2: 0.5 h / 25 °C / Inert atmosphere; Large scale reaction 5.3: 5 - 15 °C / Inert atmosphere; Large scale reaction View Scheme
Multi-step reaction with 4 steps 1.1: chlorosulfonic acid / Inert atmosphere 2.1: triethylamine / dichloromethane / -10 - 20 °C / Inert atmosphere; Large scale reaction 3.1: methanesulfonyl chloride; triethylamine / tetrahydrofuran / 20 h / -10 - 0 °C / Inert atmosphere; Large scale reaction 3.2: 0 - 25 °C / Inert atmosphere; Large scale reaction 3.3: 0.58 h / 75 °C / Inert atmosphere; Large scale reaction 4.1: potassium carbonate / dichloromethane; water / 1 h / 20 °C / Inert atmosphere; Large scale reaction 4.2: 0.5 h / 25 °C / Inert atmosphere; Large scale reaction 4.3: 5 - 15 °C / Inert atmosphere; Large scale reaction View Scheme

4-­fluoroisoquinoline (394-67-2) → 4-fluoroisoquinoline-5-sulfonic acid (906820-10-8) + 4-fluoroisoquinoline-8-sulfonic acid (1334294-09-5)

Conditions	Yield
With sulfuric acid; sulfur trioxide at 30℃; for 4h; Inert atmosphere;
Multi-step reaction with 2 steps 1: sulfuric acid / acetone / 2 h / 0 - 10 °C / Inert atmosphere; Large scale reaction 2: sulfur trioxide / 19 h / 30 °C / Inert atmosphere View Scheme
With phosphotungstic acid; sulfuric acid; sulfur trioxide at 30℃; for 3h; Reagent/catalyst; Temperature;

4-­fluoroisoquinoline (394-67-2) → 4-fluoro-5-isoquinolinesulfonyl chloride (194032-33-2)

Conditions	Yield
Multi-step reaction with 3 steps 1.1: sulfuric acid; potassium nitrate / 12 h / 25 °C / Inert atmosphere 2.1: zinc; ammonium chloride / water; tetrahydrofuran / 5 h / 25 °C / Inert atmosphere 3.1: hydrogenchloride; sodium nitrate / water / 1 h / -15 °C / Inert atmosphere 3.2: 2 h / -5 - 0 °C View Scheme

4-­fluoroisoquinoline (394-67-2) → 4-fluoro-5-isoquinolinesulfonyl chloride (194032-33-2) + C9H5ClFNO2S

Conditions	Yield
Multi-step reaction with 2 steps 1.1: sulfuric acid / acetone / 2 h / 0 - 10 °C / Inert atmosphere; Large scale reaction 2.1: sulfur trioxide / 19 h / 30 °C / Inert atmosphere; Large scale reaction 2.2: 7 h / 30 - 70 °C / Inert atmosphere View Scheme

4-­fluoroisoquinoline (394-67-2) → 1-­bromo-4-fluoroisoquinoline (1421517-86-3)

Conditions	Yield
Multi-step reaction with 2 steps 1.1: 3-chloro-benzenecarboperoxoic acid / dichloromethane / 14 h / 0 - 20 °C 2.1: tetrabutylammomium bromide / dichloromethane / 0.17 h / 20 °C / Inert atmosphere; Molecular sieve 2.2: 20 °C / Inert atmosphere View Scheme

4-­fluoroisoquinoline (394-67-2) → 4-fluoroisoquinoline-5-amine (928664-14-6)

Conditions	Yield
Multi-step reaction with 2 steps 1: sulfuric acid; potassium nitrate / 12 h / 25 °C / Inert atmosphere 2: zinc; ammonium chloride / water; tetrahydrofuran / 5 h / 25 °C / Inert atmosphere View Scheme

Upstream product

• 1532-97-4 4-bromoisoquinoline 
• 1532-71-4 1-bromoisoquinoline 
• 1421517-86-3 1--bromo-4-fluoroisoquinoline 
• 491-30-5 1-hydroxyisoquinoline 
• 491-30-5 1-isoquinolone 
• 133745-75-2 N-fluorobis(benzenesulfon)imide 
• 23687-25-4 4-aminoisoquinoline 

Downstream Products

• 906820-09-5 4-fluoroisoquinoline sulfate 
• 1334294-10-8 C₉H₅ClFNO₂S*ClH 
• 906820-08-4 4-fluoroisoquinoline-5-sulfonyl chloride hydrochloride 
• 223644-02-8 4-fluoro-5-[[(2S)-hexahydro-2-methyl-1H-1,4-diazepin-1-yl]sulfonyl]isoquinoline hydrochloride 
• 194032-33-2 4-fluoro-5-isoquinolinesulfonyl chloride 
• 1421517-86-3 1--bromo-4-fluoroisoquinoline 
• 928664-14-6 4-fluoroisoquinoline-5-amine 

Relevant articles and documents

Synthesis method of 4-fluoroisoquinoline sulfate

The invention discloses a synthesis method of 4-fluoroisoquinoline sulfate, the synthesis method comprises the following steps: S1: putting 1-bromine isoquinoline, an NFSI reagent and acetonitrile into a reaction kettle, sufficiently and uniformly stirring, starting the reaction kettle to enable the reaction temperature to be about 60-65 DEG C, and setting the reaction time to be 6-24 hours; afterthe reaction is finished, spin-drying the organic solvent in the reaction liquid through a vacuum rotary dryer, adding water into the reaction liquid, carrying out water-phase extraction work by using dichloromethane, and combining an organic phase; then adjusting the pH value of the organic phase by using a sodium bicarbonate solution, washing the organic phase by using a sodium chloride solution after the adjustment is finished, and carrying out vacuum spin-drying on the organic phase by using a vacuum rotary dryer so as to synthesize the 1-bromo-4-fluoroisoquinoline. The method is reasonable in design, the preparation steps of the isoquinoline compound can be shortened, the production and synthesis efficiency of the isoquinoline compound can be improved, and then the market requirements are met.

A 4 - quinoline [...] -5 - synthesis of amines method (by machine translation)

The present invention provides a 4 - [...] quinoline - 5 - amine synthesis method. Synthesis method of the invention, in order to isoquinoline - 1 - ol as raw materials with Selectfluor reaction to obtain 4 - fluoro - 3 - methoxy different quinoline - 1 - ol, dissolved in HCl reaction to obtain 4 - [...] quinoline - 1 - ol, and phosphorus oxychloride reaction to obtain the 1 - chloro - 4 - [...] quinoline, under the catalysis of the catalyst 4 - [...] quinoline, and concentrated nitric acid to obtain 4 - fluoro - 5 - [...] quinoline, the final acid under the conditions of reduction to obtain the iron powder 4 - [...] quinoline - 5 - amine. The invention of 4 - [...] quinoline - 5 - amine synthesis method, route the succinct, reasonable process, low material cost, simple and easy to obtain, operation and after treatment is convenient, the total yield is high, not with the use of toxic reagents, easy to enlarge, can be 4 - [...] quinoline - 5 - amine of large-scale production. (by machine translation)

ISOQUINOLINESULFONYL DERIVATIVE AS RHO KINASE INHIBITOR

The present invention discloses a class of isoquinolinesulfonyl derivatives as RHO kinase inhibitors, and pharmaceutical compositions thereof, and relates to pharmaceutically acceptable uses thereof. Specifically, the present invention relates to a compound as represented by formula (I), or a pharmaceutically acceptable salt thereof.