394-67-2Relevant articles and documents
Synthesis method of 4-fluoroisoquinoline sulfate
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Paragraph 0010-0012, (2020/12/30)
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.
ROCK KINASE INHIBITORS
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Paragraph 0191-0193, (2020/05/29)
The present invention relates to compounds that inhibit ROCK activity. In particular, the present invention relates to compounds, pharmaceutical compositions and methods of use, such as methods of inhibiting ROCK activity and methods for treating, for example cerebral cavernous malformation syndrome (CCM) and cardiovascular diseases using the compounds and pharmaceutical compositions of the present invention.
A 4 - quinoline [...] -5 - synthesis of amines method (by machine translation)
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Paragraph 0055; 0056, (2018/10/19)
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)
METHOD FOR PRODUCING 4-FLUOROISOQUINOLINE
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Sheet 0054; 0056, (2018/06/21)
PROBLEM TO BE SOLVED: To provide a method capable of producing 4-fluoroisoquinoline more simply and in a shorter time compared to heretofore known methods. SOLUTION: Provided is a method for producing 4-fluoroisoquinoline represented by formula (1), where 1-chloro-4-fluoroisoquinoline represented by formula (9a) is reductively decomposed preferably in the presence of a palladium catalyst. Also provided is the method, where 1-chloro-4-fluoroisoquinoline represented by formula (9a) is obtained by treating 1-hydroxyisoquinoline with a fluorinating agent to obtain 4-fluoro-1-hydroxy-3-methoxy-3,4-dihydroxyisoquinoline, which is reacted with a chlorinating agent. SELECTED DRAWING: None COPYRIGHT: (C)2018,JPOandINPIT
ISOQUINOLINESULFONYL DERIVATIVE AS RHO KINASE INHIBITOR
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Paragraph 0301; 0302, (2017/06/12)
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.
Derisking the Cu-Mediated 18F-Fluorination of Heterocyclic Positron Emission Tomography Radioligands
Taylor, Nicholas J.,Emer, Enrico,Preshlock, Sean,Schedler, Michael,Tredwell, Matthew,Verhoog, Stefan,Mercier, Joel,Genicot, Christophe,Gouverneur, Véronique
supporting information, p. 8267 - 8276 (2017/06/27)
Molecules labeled with fluorine-18 (18F) are used in positron emission tomography to visualize, characterize and measure biological processes in the body. Despite recent advances in the incorporation of 18F onto arenes, the development of general and efficient approaches to label radioligands necessary for drug discovery programs remains a significant task. This full account describes a derisking approach toward the radiosynthesis of heterocyclic positron emission tomography (PET) radioligands using the copper-mediated 18F-fluorination of aryl boron reagents with 18F-fluoride as a model reaction. This approach is based on a study examining how the presence of heterocycles commonly used in drug development affects the efficiency of 18F-fluorination for a representative aryl boron reagent, and on the labeling of more than 50 (hetero)aryl boronic esters. This set of data allows for the application of this derisking strategy to the successful radiosynthesis of seven structurally complex pharmaceutically relevant heterocycle-containing molecules.
Rapid Synthesis of Aryl Fluorides in Continuous Flow through the Balz–Schiemann Reaction
Park, Nathaniel H.,Senter, Timothy J.,Buchwald, Stephen L.
supporting information, p. 11907 - 11911 (2016/11/17)
The Balz–Schiemann reaction remains a highly utilized means for preparing aryl fluorides from anilines. However, the limitations associated with handling aryl diazonium salts often hinder both the substrate scope and scalability of this reaction. To address this, a new continuous flow protocol was developed that eliminates the need to isolate the aryl diazonium salts. The new process has enabled the fluorination of an array of aryl and heteroaryl amines.
Pd-catalyzed nucleophilic fluorination of aryl bromides
Lee, Hong Geun,Milner, Phillip J.,Buchwald, Stephen L.
supporting information, p. 3792 - 3795 (2014/04/03)
On the basis of mechanism-driven reaction design, a Pd-catalyzed nucleophilic fluorination of aryl bromides and iodides has been developed. The method exhibits a broad substrate scope, especially with respect to nitrogen-containing heteroaryl bromides, and proceeds with minimal formation of the corresponding reduction products. A facilitated ligand modification process was shown to be critical to the success of the reaction.
SULFONAMIDE COMPOUND
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Page/Page column 46, (2010/04/30)
A compound represented by the formula (1) [A represents a nitrogen-containing saturated ring; m represents an integer of 0 to 2; n represents an integer of 1 to 4; G1 represents hydrogen atom, chlorine atom, hydroxyl group, an alkoxy group, or amino group; G2 represents a halogen atom, hydroxyl group, cyano group, carboxy group, an alkyl group, an alkenyl group, and the like; G3 represents hydrogen atom, a halogen atom, hydroxyl group, cyano group, carboxy group, an alkyl group, an alkenyl group, and the like; G4 represents hydroxyl group, or —N(R1)(R2) (R1 and R2 represent hydrogen atom, an alkyl group, an aralkyl group, an alkenyl group, an alkynyl group, or a saturated heterocyclic group); G5 is a substituent on a ring-constituting carbon atom of A, and represents hydrogen atom, fluorine atom, or an alkyl group] or a salt thereof, or a derivative thereof that is a prodrug, which potently inhibits Rho kinase.
Sulfonamide compound
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Page/Page column 101, (2009/03/07)
A compound represented by the formula (1) [A represents a nitrogen-containing saturated ring; m represents an integer of 0 to 2; n represents an integer of 1 to 4; G1 represents hydrogen atom, chlorine atom, hydroxyl group, an alkoxy group, or amino group; G2 represents a halogen atom, hydroxyl group, cyano group, carboxy group, an alkyl group, an alkenyl group, an alkynyl group, an alkoxy group, an alkylthio group, an amino group, an alkylsulfinyl group, an alkylsulfonyl group, or an aryl group; G3 represents hydrogen atom, a halogen atom, hydroxyl group, cyano group, carboxy group, an alkyl group, an alkenyl group, an alkynyl group, an alkoxy group, an alkylthio group, an amino group, an alkoxycarbonyl group, an acyl group, an acyloxy group, an alkylsulfinyl group, an alkylsulfonyl group, or an aryl group; Y represents a single bond, or —C(R3)(R4)— (R3 and R4 represent hydrogen atom, or an alkyl group, or alkylene groups which combine together to form a saturated hydrocarbon ring group); G4 represents hydroxyl group (Y is a single group), or —N(R1)(R2) (R1 and R2 represent hydrogen atom, an alkyl group, an aralkyl group, an alkenyl group, an alkynyl group, a saturated heterocyclic group, an alkylsulfonyl group, an acyl group, or an amidino group); G5 is a substituent on a ring-constituting carbon atom of A, and represents hydrogen atom, fluorine atom, or an alkyl group] or a salt thereof, or a derivative thereof that is a prodrug, which potently inhibits Rho kinase.
