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Upstream product

• 2398-37-0 3-methoxyphenyl bromide 
• 766-85-8 3-methoxy-1-iodobenzene 
• 79-05-0 Propionamid 
• 79-03-8 propionyl chloride 
• 536-90-3 m-Anisidine 

Downstream Products

• 913613-84-0 7-methoxy-3-methylquinolin-2(1H)-one 

Relevant academic research and scientific papers

Copper-catalyzed Goldberg-type C-N coupling in deep eutectic solvents (DESs) and water under aerobic conditions

An efficient and selectiveN-functionalization of amides is first reportedviaa CuI-catalyzed Goldberg-type C-N coupling reaction between aryl iodides and primary/secondary amides run either in Deep Eutectic Solvents (DESs) or water as sustainable reaction media, under mild and bench-type reaction conditions (absence of protecting atmosphere). Higher activities were observed in an aqueous medium, though the employment of DESs expanded and improved the scope of the reaction to include also aliphatic amides. Additional valuable features of the reported protocol include: (i) the possibility to scale up the reaction without any erosion of the yield/reaction time; (ii) the recyclability of both the catalyst and the eutectic solvent up to 4 consecutive runs; and (iii) the feasibility of the proposed catalytic system for the synthesis of biologically active molecules.

Development and Kilogram-Scale Synthesis of a D2/5-HT2A Receptor Dual Antagonist (±)-SIPI 6360

The kilogram-scale synthesis of a D2/5-HT2A receptor dual antagonist (±)-SIPI 6360 was developed as an alternative treatment for schizophrenia. Specifically, three conditions were modified and optimized, including the Vilsmeier condi

Rapid and efficient copper-catalyzed finkelstein reaction of (hetero)aromatics under continuous-flow conditions

A general, rapid, and efficient method for the copper-catalyzed Finkelstein reaction of (hetero)aromatics has been developed using continuous flow to generate a variety of aryl iodides. The described method can tolerate a broad spectrum of functional groups, including N-H and O-H groups. Additionally, in lieu of isolation, the aryl iodide solutions were used in two distinct multistep continuous-flow processes (amidation and Mg-I exchange/nucleophilic addition) to demonstrate the flexibility of this method.

Synthesis, biological evaluation and mechanism study of a class of cyclic combretastatin A-4 analogues as novel antitumour agents

In the course of our search for novel antitumor agents, a series of cyclic combretastatin A-4 (CA-4) analogues bearing an amide group, A-B or B-C ring condensation, and CC or CN bond in the B ring were designed, synthesized and identified as new microtubule inhibitors. The structure-activity relationship (SAR) studies showed that the hexa-cyclic compounds bearing B-C ring condensation, containing a CC bond in the B ring (4a) provided excellent antiproliferative activities at nanomolar concentrations against various cancer cell lines (IC50 = 46-80 nM). 4a inhibited tubulin assembly at a micromolar range (IC50 = 2.56 ± 0.15 μM) as evidenced by a molecular docking study, which revealed that 4a exerted tubulin polymerisation inhibitory activity by binding to the colchicine binding site of tubulin. Further molecular biology studies showed that 4a disrupted intracellular microtubule polymerisation and thus induced G2/M phase arrest and apoptotsis in A549 cells. Altogether, these results we obtained can guide the design of novel potent molecules for future development.

The convenient aqueous synthesis and biological evaluation of ortho-(3,4,5-trimethoxybenzoyl)-acetanilides as novel anti-cancer agents

A series of new ortho-(3,4,5-trimethoxybenzoyl)-acetanilides were synthesised by the cross-coupling reaction catalyzed with Pd catalyst in aqueous medium, with polyethylene glycol as additive under very mild conditions. The evaluation of these compounds as tubulin polymerization inhibitors indicated that most of these compounds were potential anti-cancer agents. Among them, compound 13, 2-hydroxy-N-(5-methoxy-2-(3,4,5-trimethoxy benzoyl)phenyl) acetamide exhibited excellent antiproliferative activity against various human cancer cell lines (GI50= 71 nM for human HeLa cell line), and good activity for inhibiting tubulin polymerization (IC50= 2.94 μM). The mechanism study indicated that compound 13 could arrest cell-cycle progression at the mitosis phase, block the formation of cdc2/cyclin B1 complex, down-regulate the p-Cdc 25C and the anti-apoptotic proteins Bcl-2 and Bcl-XL, and up-regulate the pro-apoptotic proteins Bax and Bad. This journal is

PROTECTIVE AGENT FOR RETINAL NEURONAL CELL COMPRISING INDAZOLE DERIVATIVE AS ACTIVE INGREDIENT

As a result of intensive studies for the purpose of finding a new medicinal use of an indazole derivative, it was found that an indazole derivative inhibits glutamate-induced retinal neuronal cell death in rat fetal retinal neuronal cells, in other words, the indazole derivative acts directly on the retinal neuronal cells and exhibits an effect of protecting retinal neuronal cells. Accordingly, the indazole derivative is useful for the prevention or treatment of an eye disease associated with retinal neuronal cell damage or retinal damage.