16576-24-2

Upstream product

• 119-65-3 isoquinoline 
• 106-43-4 para-chlorotoluene 
• 104-88-1 4-chlorobenzaldehyde 
• 1532-71-4 1-bromoisoquinoline 
• 873-76-7 para-Chlorobenzyl alcohol 
• 7099-88-9 4-chlorophenylglyoxylic acid 
• 1532-72-5 isoquinoline N-oxide 
• 706-07-0 1-chloro-4-(2-nitrovinyl)benzene 
• 1198-30-7 1-isoquinolinecarbonitrile 
• 352-33-0 1-Chloro-4-fluorobenzene 

Downstream Products

• 82319-68-4 2-amino-1-(4-chlorobenzoyl)-isoquinolinium-p-toluene sulfonate 

Relevant academic research and scientific papers

Metal-free decarboxylative acylation of isoquinolines using α-keto acids in water

An efficient method for acylation of isoquinolines has been developed using α-ketoacids under metal- and additive-free conditions in water. The protocol involves C(sp2)–H functionalization of isoquinolines providing an easy access to C1-benzoylated isoquinolines, which constitute the core structure of a number of biological active compounds and serve as key intermediate in the synthesis of many alkaloids.

The synergistic effect of self-assembly and visible-light induced the oxidative C-H acylation of N-heterocyclic aromatic compounds with aldehydes

Constructing carbon-carbon bonds through oxidative cross-coupling between two hydrocarbon compounds is regarded as a foundational issue in green chemistry. High atom-economy and mild conditions are long term pursued goals in this field. Herein, we develop

Transition-Metal-Free Acylation of Quinolines and Isoquinolines with Arylmethanols via Oxidative Cross-Dehydrogenative Coupling Reactions

An efficient acylation of quinolines and isoquinolines is described by use of arylmethanols as the acylating agents through a C-C bond formation via an oxidative cross-dehydrogenative coupling (CDC) strategy. This C-aroylation reaction was carried out by use of K2S2O8 as oxidant and methyltrioctylammonium chloride (Aliquat 336) as a transfer agent in MeCN at 80 °C under transition-metal-free conditions.

Synthetic method for drug intermediate diaryl ketone compound

The invention relates to a synthetic method for a diaryl ketone compound which can be used as a drug intermediate and is shown as a formula (III) which is described in the specification. The method comprises a step of reacting a compound (I) as described in the specification with a compound (II) as described in the specification in a nitrogen atmosphere and organic solvent in the presence of a catalyst, an oxidizing agent, alkali and a promoter so as to obtain the compound as shown in the formula (III). In the formula (III), R1, R2 and R3 are independently selected from a group consisting of H, C1-6 alkyl groups, C1-6 alkyloxy groups, halogen and nitro groups; and X is halogen. According to the method, through selection of an appropriate substrate and usage of a reaction system composed of the catalyst, the oxidizing agent, the alkali and the promoter, high yield of the target product, i.e., the diaryl ketone compound, is realized; and a brand novel synthetic method is provided for the compound, and the synthetic method has wide market application prospects.

Palladium(II)-catalyzed C-C and C-O bond formation for the synthesis of C1-benzoyl isoquinolines from isoquinoline: N -oxides and nitroalkenes

C1-Benzoyl isoquinolines can be generated via a palladium(ii)-catalyzed C-C and C-O coupling of isoquinoline N-oxides with aromatic nitroalkenes. The reaction proceeds through remote C-H bond activation and subsequent intramolecular oxygen atom transfer (OAT). In this reaction, the N-O bond was designed as a directing group in the C-H bond activation as well as the source of an oxygen atom.

TBHP/TFA mediated oxidative cross-dehydrogenative coupling of N-heterocycles with aldehydes

An effective and metal-free oxidative cross-dehydrogenative coupling (CDC) of N-heterocycles with diverse aldehydes has been established in the presence of TBHP/TFA. The scope with respect to aldehyde and N-heterocycle components is broad, allowing facile synthesis of a broad range of structurally diverse C1-acyl substituted heterocycles in good efficiency.

Regiospecific benzoylation of electron-deficient n -heterocycles with methylbenzenes via a minisci-type reaction

A regioselective cross-dehydrogenative coupling between electron-deficient N-heterocycles (isoquinoline, quinolines, and quinoxalines) and methylbenzenes leading to regiospecific C-aroylation has been accomplished using AlCl3 as the catalyst in

C1-Benzyl and benzoyl isoquinoline synthesis through direct oxidative cross-dehydrogenative coupling with methyl arenes

An oxidative cross-dehydrogenative coupling (CDC) of isoquinolines with methyl arenes has been developed, allowing for the facile synthesis of a broad range of structurally diverse C1-benzyl and -benzoyl isoquinolines. The direct use of readily available methyl arenes as coupling partners avoids unproductive steps for preactivating the functional group installation, and is therefore attractive. The method exhibits excellent chemoselectivity, affording exclusive benzylated products in the presence of DTBP and a catalytic amount of Y(OTf)3, and yielding benzoylated ones with TBHP and a catalytic amount of MnO2.

Synthesis of quinolinyl and isoquinolinyl phenyl ketones as novel agonists for the cannabinoid CB2 receptor

A series of quinolinyl and isoquinolinyl phenyl ketones was synthesized and their CB2 receptor-dependent G-protein activities were determined using the [35S]GTPγS binding assay. Both quinoline and isoquinoline derivatives exhibited similar CB2 receptor agonist activity, the most potent ligands being the 2-(Me2N)-phenyl substituted derivatives, which were also full agonists at the CB2-receptor.

Condensed as-triazine derivatives and method of using the same

The invention relates to new condensed as-triazine derivatives of the general formula (I) STR1 wherein Z represents a buta-1,3-dienyl group or a group of the formula (a), (b), (c) or (d) STR2 R1 denotes a C1-10 alkyl group, an oxo gr