30024-74-9

Upstream product

• 274-09-9 Methylenedioxybenzene 
• 20850-43-5 5-(chloromethyl)-1,3-benzodioxole 
• 94-59-7 1-allyl-3,4-methylenedioxybenzene 
• 25054-53-9 3,4-(methylenedioxy)benzoyl chloride 
• 64-18-6 formic acid 
• 10584-67-5 1-dichloromethyl-3,4-methylenedioxybenzene 
• 2861-28-1 1,3-benzodioxole-5-acetic acid 
• 62396-98-9 benzo[1,3]dioxol-5-yl-oxo-acetic acid 
• 27738-46-1 3,4-(methylenedioxy)mandelic acid 
• 406190-94-1 piperonylic acid-(N'-benzenesulfonyl-hydrazide) 
• 623-11-0 1-methyl-4-nitrosobenzene 
• 98-09-9 benzenesulfonyl chloride 
• 64-17-5 ethanol 
• 64-19-7 acetic acid 

Downstream Products

• 51003-16-8 trans-1-(3,4-methylenedioxyphenyl)-2-phenylethylene 
• 42307-51-7 (Z)-3-(3,4-methylenedioxyphenyl)-2-phenylprop-2-enoic acid 
• 42518-30-9 5-(Z)-benzo[1,3]dioxol-5-ylmethylene-3-phenyl-thiazolidine-2,4-dione 
• 158117-67-0 2,4-dinitro-3',4'-methylenedioxystilbene 
• 35546-62-4 benzo[1,3]dioxol-5-ylmethylene-[1,2,4]triazol-4-yl-amine 
• 77669-23-9 (E)-2-(2-(benzo[d][1,3]dioxol-5-yl)vinyl)quinoline 
• 28824-65-9 5-Piperonyliden-2-thiohydantoin 
• 6318-41-8 AS041164 
• 28824-66-0 (5Z)-5-(1,3-benzodioxol-5-ylmethylene)-2-thioxo-1,3-thiazolidin-4-one 
• 28824-66-0 5-(1,3-benzodioxol-5-ylmethylidene)-2-thioxo-1,3-thiazolidin-4-one 
• 60546-62-5 6-bromopiperonylic acid 
• 15930-53-7 6-bromo-3,4-methylenedioxybenzaldehyde 
• 1400815-07-7 (E)-N'-(benzo[d][1,3]dioxol-5-ylmethylene)thiophene-2-carbohydrazide 
• 17253-14-4 2-benzo[1,3]dioxol-5-yl-indan-1,3-dione 

Relevant academic research and scientific papers

Aerobic oxidation of alcohols enabled by nitrogen-doped copper nanoparticle catalysts

Heterogeneous nitrogen-doped carbon-incarcerated copper nanoparticle catalysts have been developed. The catalysts promoted the oxidation of alcohols to the corresponding aldehydes, including aliphatic substrates, in high yield in the presence of an N-oxyl

A “universal” catalyst for aerobic oxidations to synthesize (hetero)aromatic aldehydes, ketones, esters, acids, nitriles, and amides

Functionalized (hetero)aromatic compounds are indispensable chemicals widely used in basic and applied sciences. Among these, especially aromatic aldehydes, ketones, carboxylic acids, esters, nitriles, and amides represent valuable fine and bulk chemicals, which are used in chemical, pharmaceutical, agrochemical, and material industries. For their synthesis, catalytic aerobic oxidation of alcohols constitutes a green, sustainable, and cost-effective process, which should ideally make use of active and selective 3D metals. Here, we report the preparation of graphitic layers encapsulated in Co-nanoparticles by pyrolysis of cobalt-piperazine-tartaric acid complex on carbon as a most general oxidation catalyst. This unique material allows for the synthesis of simple, functionalized, and structurally diverse (hetero)aromatic aldehydes, ketones, carboxylic acids, esters, nitriles, and amides from alcohols in excellent yields in the presence of air.

Nickel(II)-Catalyzed Selective (E)-Olefination of Methyl Heteroarenes Using Benzyl Alcohols via Acceptorless Dehydrogenative Coupling Reaction

An efficient catalytic protocol for the synthesis of selective (E)-olefins by the newly synthesized nickel complexes via greener acceptorless dehydrogenative coupling methodology is presented. Two nickel(II) N, S chelating complexes were structurally characterized with the aid of spectral and single crystal X-ray diffraction methods. Olefination of 2-methylheteroarenes with benzyl alcohols via acceptorless dehydrogenative coupling is achieved by inexpensive nickel(II) catalysts. The present olefination protocol is simple and furnishes the desired 2-alkenylheteroarenes in 35 h and yields in the range of 40–93 %. The dehydrogenative coupling reaction proceeds via the generation of an aldehyde intermediate and produces water and hydrogen as sole by-products. The wide substrate scope of this catalytic reaction covered the synthesis of drug intermediates.

The development of novel cytochrome P450 2J2 (CYP2J2) inhibitor and the underlying interaction between inhibitor and CYP2J2

Human Cytochrome P450 2J2 (CYP2J2) as an important metabolic enzyme, plays a crucial role in metabolism of polyunsaturated fatty acids (PUFAs). Elevated levels of CYP2J2 have been associated with various types of cancer, and therefore it serves as a potential drug target. Herein, using a high-throughput screening approach based on enzymic activity of CYP2J2, we rapidly and effectively identified a novel natural inhibitor (Piperine, 9a) with IC50 value of 0.44 μM from 108 common herbal medicines. Next, a series of its derivatives were designed and synthesised based on the underlying interactions of Piperine with CYP2J2. As expected, the much stronger inhibitors 9k and 9l were developed and their inhibition activities increased about 10 folds than Piperine with the IC50 values of 40 and 50 nM, respectively. Additionally, the inhibition kinetics illustrated the competitive inhibition types of 9k and 9l towards CYP2J2, and K i were calculated to be 0.11 and 0.074 μM, respectively. Furthermore, the detailed interaction mechanism towards CYP2J2 was explicated by docking and molecular dynamics, and our results revealed the residue Thr114 and Thr 315 of CYP2J2 were the critical sites of action, moreover the spatial distance between the carbon atom of ligand methylene and Fe atom of iron porphyrin coenzyme was the vital interaction factor towards human CYP2J2.

A NIR fluorescent probe for fatty acid amide hydrolase bioimaging and its application in development of inhibitors

Fatty acid amide hydrolase (FAAH) is primarily responsible for the inactivation of fatty acid ethanolamide (FAE) and is involved in a variety of biological functions related to diseases of the nervous system. Herein, we developed a highly selective and sensitive FAAH-activated near-infrared fluorescent probe named DAND and achieved the real-time detection and imaging of FAAH activity in complex biosystems. Moreover, a visual high-throughput screening method was established using DAND, piperine was identified as a novel inhibitor of FAAH. Based on the interaction of piperine with FAAH, a more potent FAAH inhibitor (11f) was designed and synthesized which possessed an IC50 value of 0.65 μM. Furthermore, 11f could attenuate the liposaccharide (LPS)-induced activation of BV2 cells, exhibiting an excellent anti-inflammatory activity. These results indicated that DAND could be used as a promising molecular tool for exploring FAAH activity and for rapidly screening potential FAAH inhibitors. In addition, piperine and its derivatives could serve as potential candidate drugs for the treatment of neurodegenerative diseases in the future.

A method of synthesis of piperonolamine

The present invention belongs to the field of organic chemical synthesis, specifically relates to a synthesis method of piperine, comprising: using catechol as a raw material to prepare piperonaldehyde; β - nitro-3,4-dioxenosylstyrene prepared with piperonaldehyde; β - nitro -3,4-dioxenesimethylenestyrene to obtain piperine ethylamine. Among them, the preparation of piperaldehyde from catechol as raw materials includes two ways: (1) catechol→3,4-dihydroxymandelic acid→3,4-dihydroxybenzaldehyde→ piperaldehyde; (2) catechol→ piperine ring → piperine. The raw materials used in the present invention are safe and readily available, low cost; the reaction conditions are mild, the operation is simple, the chemical yield is high, and the intermediate reagents are easy to recover; suitable for industrial production.

A synthetic preparation method for small carbags hydrochloric acid

The present invention belongs to the field of organic chemistry, relates to a method of synthesizing berberine hydrochloride, comprising: S1: with 5-halo-o-quinoastearaldehyde and piperine ethylamine to obtain N- [2-(3,4-dimethoxyphenyl-5-yl) ethyl] -1- (5-halo-2,3-dimethoxybenzyl) methylimide; S2: to obtain 2- (3,4-diimoxyphenyl) -N- (5-bromo-2,3-dimethoxybenzyl) ethylamine; S3: to obtain 2-(3,4-dimethoxyphenyl) -N- (5-bromo-2 S4: to obtain 12-halogenated berberine derivative; S5: to obtain berberine. The present invention is free from the application of the by-product o-vanillin synthesis of o-resveratal raw material constraints, synthesis of 5- substitute o-resveratal and piperine ethylamine, and the use of the two preparation of berberine hydrochloride, with raw materials readily available, mild reaction conditions, easy to operate, high chemical yield, low cost and other advantages.

One-Pot Direct Oxidation of Primary Amines to Carboxylic Acids through Tandem ortho-Naphthoquinone-Catalyzed and TBHP-Promoted Oxidation Sequence

Biomimetic oxidation of primary amines to carboxylic acids has been developed where the copper-containing amine oxidase (CuAO)-like o-NQ-catalyzed aerobic oxidation was combined with the aldehyde dehydrogenase (ALDH)-like TBHP-mediated imine oxidation protocol. Notably, the current tandem oxidation strategy provides a new mechanistic insight into the imine intermediate and the seemingly simple TBHP-mediated oxidation pathways of imines. The developed metal-free amine oxidation protocol allows the use of molecular oxygen and TBHP, safe forms of oxidant that may appeal to the industrial application.

USE OF HETEROCYCLIC DERIVATIVES WITH CARDIOMYOCYTE PROLIFERATION ACTIVITY FOR TREATMENT OF HEART DISEASES

Provided herein is the use of heterocyclic derivatives with cardiomyocyte proliferation activity for treatment of heart diseases. Specifically, disclosed is the use of compounds of formula (I) or a pharmaceutically acceptable salt, a solvate, a stereoisomer or a prodrug thereof; and application thereof. Definition of each group in the formula can be found in the specification for details.

NOVEL HETEROCYCLIC DERIVATIVES WITH CARDIOMYOCYTE PROLIFERATION ACTIVITY FOR TREATMENT OF HEART DISEASES

Provided are novel heterocyclic derivatives with cardiomyocyte proliferation activity for treatment of heart diseases. Specifically, provided are the compounds of formula (I) or pharmaceutically acceptable salts, stereoisomers, solvates or prodrugs, prepa