140202-00-2

Usage

Uses

Used in Organic Synthesis:
Trifluoro-methanesulfonic acid isoquinolin-5-yl ester is used as a reagent in organic synthesis for facilitating various chemical reactions. Its strong acidic properties make it a valuable catalyst in processes that require acidic conditions, enhancing the efficiency and selectivity of the reactions.
Used in Pharmaceutical Research and Drug Development:
In the pharmaceutical industry, Trifluoro-methanesulfonic acid isoquinolin-5-yl ester is employed as a key intermediate in the synthesis of potential drug candidates. Its unique chemical properties allow for the exploration of new molecular structures and therapeutic agents, contributing to the advancement of medicinal chemistry.
Used in Chemical Reactions:
Trifluoro-methanesulfonic acid isoquinolin-5-yl ester is used as a catalyst in chemical reactions that necessitate acidic conditions. Its strong acidity enables it to facilitate reactions that may otherwise be slow or inefficient, thereby improving the overall reaction kinetics and yield.
Used in Research and Development:
In the field of research and development, Trifluoro-methanesulfonic acid isoquinolin-5-yl ester is utilized as a tool to investigate new chemical pathways and explore novel synthetic methods. Its versatility in various reactions makes it a valuable asset in the pursuit of scientific discovery and innovation.

Upstream product

• 358-23-6 trifluoromethylsulfonic anhydride 
• 2439-04-5 5-hydroxyisoquinoline 
• 1493-13-6 trifluorormethanesulfonic acid 
• 456-64-4 phenyl trifluoromethanesulfonamide 

Downstream Products

• 1363958-80-8 2,3,4,5,6-pentafluoro-2'-methoxy-5'-methyl-1,1'-biphenyl 
• 919120-74-4 (3R)-N-[1-(3-nitrobenzyl)-3-pyrrolidyl]-N-(5-isoquinolyl)amine 

Relevant academic research and scientific papers

Scope of direct arylation of fluorinated aromatics with aryl sulfonates

The scope and limitations of direct arylation of fluorinated aromatics with aryl sulfonates was examined. Pd(OAc)2, in the presence of MePhos and KOAc in THF, efficiently catalyzed the direct arylation of fluoro aromatics with aryl triflates un

ANTIMICROBIAL AGENTS

The invention provides a compound of formula I:or a salt thereof, wherein R3-R8 and X and Y have any of the values described in the specification, as well as compositions comprising a compound of formula I. The compounds are useful as antibacterial agents.

Design and synthesis of rho kinase inhibitors (III)

The structure-activity relationship of Rho kinase inhibitors bearing an isoquinoline scaffold was studied. N-(1-Benzyl-3-pyrrolidyl)-N-(5-isoquinolyl)amine analogues were optimized with respect to their inhibitory potencies for the enzyme and for chemotaxis. The potent analogues were further evaluated by an ex vivo test in which the selected compounds were orally administered to rats, and the Rho kinase inhibitory potency observed in the rat serum was evaluated 3 h after the administration. Compound 23g showed a high level of Rho kinase inhibitory activity in the rat serum and was stable in an in vitro metabolic test using a microsomal cytochrome preparation. The (R)-isomer of 23g displayed a higher level of inhibitory potency than the (S)-isomer in a cell-free kinase assay and in the cell migration assay (IC50ENZ = 25 nM and IC50MCP = 1 μ M). The (R)-isomer successfully inhibited the phosphorylation of MBS (myosin-binding subunit) in cells.

ISOQUINOLINE DERIVATIVES HAVING KINASAE INHIBITORY ACTIVITY AND DRUGS CONTAINING THE SAME

An objective of the present invention is to provide compounds having Rho kinase inhibitory activity and useful for the treatment of diseases mediated by Rho kinase. The compounds according to the present invention are those represented by formula (I) or pharmaceutically acceptable salts or solvates thereof: wherein Q represents phenyl, pyridyl, pyrrolyl, thienyl, or furyl; these groups are optionally substituted by one or two halogens or alkyl, nitro, or amino groups; and p is 2 or 3.

ARYLPIPERAZINYL-CYCLOHEXYL INDOLE DERIVATIVES FOR THE TREATMENT OF DEPRESSION

Compounds are provided which are useful for the treatment of serotonin-affected neurological disorders which comprise (I) wherein: Ra, R1, R2 and R3 are each, independently, hydrogen, or a substituent selected from halogen, CF3, alkyl, alkoxy, MeSO2, amino or aminocarbonyl (each optionally substituted by one or two groups selected from alkyl and benzyl) carboxy, or alkoxycarbonyl; or two adjacent of Ra and R1-4 together can form a 5-7 membered carbocyclic or heterocyclic ring which is optionally substituted by a substituent defined above; R4 is hydrogen, halogen, or alkyl; R5 is hydrogen, alkyl, arylalkyl, or aryl; R6 is hydrogen, halogen, CF3, CN, carbamide, alkoxy or benzyloxy; X1, X2 and X3 are each carbon or one of X1, X2 or X3 may be nitrogen; Y is CH or nitrogen; and Z is carbon or nitrogen; or pharmaceutically acceptable salts thereof.

Kinase inhibitors

Compounds having the formula are useful for inhibiting protein kinases. Also disclosed are compositions which inhibit protein kinases and methods of inhibiting protein kinases in a patient.

Kinase inhibitors

Compounds having the formula are useful for inhibiting protein kinases. Also disclosed are compositions which inhibit protein kinases and methods of inhibiting protein kinases in a patient.

Generation of N-Methyl-D-aspartate Agonist and Competitive Antagonist Pharmacophore Models. Design and Synthesis of Phosphonoalkyl-Substituted Tetrahydroisoquinolines as Novel Antagonists

The preparation and binding affinity of a series of tetrahydroisoquinoline carboxylic acids at the N-methyl-D-aspartate (NMDA) subtype of the glutamate receptor is described, together with a molecular modeling analysis of NMDA agonists and antagonists.Usi