33930-64-2

Upstream product

• 491-30-5 1-isoquinolone 
• 3951-95-9 4-bromo-1,2-dihydroisoquinolin-1-one 
• 100-39-0 benzyl bromide 
• 119-65-3 isoquinoline 
• 23277-04-5 2-benzylisoquinolin-2-ium bromide 
• 1532-97-4 4-bromoisoquinoline 
• 108-88-3 toluene 
• 34784-02-6 3-bromoisoquinoline 
• 13605-95-3 N-benzyl-1,2,3,4-tetrahydroisoquinoline 
• 59168-21-7 2-benzyl-1-(2H)-isoquinoline ketone 

Downstream Products

• 1558050-02-4 2-benzyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)isoquinolin-1-one 
• 1616401-73-0 2-benzyl-4-((3,4,5-trimethoxyphenyl)amino)isoquinolin-1(2H)-one 
• 1616401-70-7 2-benzyl-4-(4-hydroxy-3-methoxyphenyl)isoquinolin-1(2H)-one 
• 1616401-69-4 2-benzyl-4-(3,4,5-trimethoxyphenyl)isoquinolin-1(2H)-one 
• 1616401-67-2 2-benzyl-4-(3,4-dimethoxyphenyl)isoquinolin-1(2H)-one 
• 1616401-68-3 2-benzyl-4-(3,5-dimethylisoxazol-4-yl)isoquinolin-1(2H)-one 

Relevant academic research and scientific papers

Oxidation of the inert sp3C-H bonds of tetrahydroisoquinolines through C-H activation relay (CHAR): construction of functionalized isoquinolin-1-ones

A TBN/O2-initiated oxidation of the relatively inert 3,4-C-H bonds of THIQs was accomplished, in which the existence of an α-phosphoric ester group is crucial to enable dioxygen trapping and intramolecular HAT (C-H activation relay,CHAR), reali

Light-driven selective aerobic oxidation of (iso)quinoliniums and related heterocycles

Selective C1-H/C4-H carbonylation of N-methylene iminium salts, catalyzed by visible-light photoredox and oxygen in the air, has been reported. A ruthenium complex acts as a chemical switch to conduct two different reaction pathways and to afford two diff

Visible-Light-Induced Controlled Oxidation of N-Substituted 1,2,3,4-Tetrahydroisoquinolines for the Synthesis of 3,4-Dihydroisoquinolin-1(2H)-ones and Isoquinolin-1(2H)-ones

A visible light-rose bengal-TBHP mediated, controlled oxidation of N-substituted 1,2,3,4-tetrahydroisoquinolines is developed for the synthesis of 3,4-dihydroisoquinolin-1(2H)-ones and isoquinolin-1(2H)-ones. The present method feature's a broad substrate scope, good functional group tolerances, and the products were prepared in good to excellent yields. The developed methodology further demonstrated in the synthesis of isoindolo[2,1-b] isoquinolin-5(7H)-one (topoisomerase-I inhibitor). (Figure presented.).

Base-promoted aerobic oxidation of: N -alkyl iminium salts derived from isoquinolines and related heterocycles

Potassium tert-butoxide-promoted aerobic oxidation of N-alkyl iminium salts is reported. The reaction is atom-economical and environmentally friendly. Iminium salts derived from isoquinoline, quinoline, phenanthridine, phenanthroline, and phthalazine were successfully transformed into their corresponding unsaturated lactams with up to 95% yield under mild conditions in the absence of photocatalysts and metallic or organic catalysts. Owing to the general substrate scope, low cost, feasibility of scale up, wide availability of reagents, and green reaction conditions, this method shows great potential for preparing isoquinolones and related compounds. The method was applied for atom- and step-economical total synthesis of natural products such as norketoyobyrine.

Copper-Mediated Oxidative Functionalization of C(sp3)-H Bonds with Isoquinolines: Two-Step Synthesis of 5-Oxaprotoberberinones

A copper-mediated oxidative functionalization of C(sp3)-H bonds with isoquinolines via a radical process without ligands was achieved. The present system exhibits a novel pathway for the preparation of N-alkyl (benzyl) isoquinolin-1(2H)-ones in moderate to high yields. In addition, this procedure provides a simple method to afford 5-oxaprotoberberinones and their derivatives in two steps.

Iodine-Catalyzed Oxidative Functionalization of Azaarenes with Benzylic C(sp3)-H Bonds via N-Alkylation/Amidation Cascade: Two-Step Synthesis of Isoindolo[2,1-b]isoquinolin-7(5H)-one

An efficient and practical iodine-catalyzed oxidative functionalization of azaarenes with benzylic C-H bonds via an N-alkylation and amidation cascade is developed to provide isoquinolin-1(2H)-ones. This method utilizes readily available unfunctionalized azaarenes and methylarenes as starting materials and proceeds under metal-free conditions with good to excellent yields, avoiding the use of expensive noble metal catalysts and generation of halide and metal wastes. The synthetic utility of this reaction is exemplified by the concise, two-step synthesis of isoindolo[2,1-b]isoquinolin-7(5H)-one.

Novel Heterocyclic Compounds as Bromodomain Inhibitors

The present disclosure relates to compounds, which are useful for inhibition of BET protein function by binding to bromodomains, and their use in therapy.

Discovery of isoquinolinone indole acetic acids as antagonists of chemoattractant receptor homologous molecule expressed on TH2 cells (CRTH2) for the treatment of allergic inflammatory diseases

Previously we reported the discovery of CRA-898 (1), a diazine indole acetic acid containing CRTH2 antagonist. This compound had good in vitro and in vivo potency, low rates of metabolism, moderate permeability, and good oral bioavailability in rodents. H