71955-53-8

Upstream product

• 506-59-2 N,N-dimethylammonium chloride 
• 1989-53-3 2,6-dimethoxybenzoyl chloride 
• 1466-76-8 2-6-dimethoxybenzoic acid 
• 125700-67-6 O-(benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium tetrafluoroborate 
• 124-40-3 dimethyl amine 
• 68-12-2 N,N-dimethyl-formamide 

Downstream Products

• 60237-95-8 2,6-dihydroxy-benzoic acid dimethylamide 

Relevant academic research and scientific papers

POCl3 promoted metal-free synthesis of tertiary amides by coupling of carboxylic acids and N,N-disubstituted formamides

Herein we report a robust and synthetically useful catalyst-free amination methodology by the coupling of carboxylic acids and N-substituted formamides using POCl3 as a promoter. Versatile amides with a wide array of substituent groups were prepared within only 1 h in good to excellent yields. And even multi-substituted aromatic carboxylic acids could give the desired products with satisfactory results.

FeCl3 catalyzed amide compound synthesis method

The invention relates to an FeCl3 catalyzed amide compound synthesis method. According to the synthesis method, carboxylic acid and N-substituted formamide are employed to synthesize an amide compound under the catalysis of FeCl3. The synthesis method provided by the invention has the characteristics of mild conditions, high reaction efficiency, and wide applicability to substrates of different functional groups. The amide compound efficiently constructed by the invention is an important skeleton of many organic molecules, drugs, proteins and bioactive molecules. The synthesis method provided by the invention provides a widely applicable preparation method for synthesis of the compounds.

Pd(PPh3)4 catalyzed amide compound synthesis method

The invention relates to a Pd(PPh3)4 catalyzed amide compound synthesis method. The synthesis method takes carboxylic acid as the substrate, and adopts N-substituted formamide as the amine source to synthesize an amide compound under the catalysis of Pd(PPh3)4. The method is widely applicable to substrates with different functional groups. The amide compound efficiently constructed by the invention is an important skeleton of many organic molecules, drugs, peptides, bioactive molecules and natural products. The synthesis method provided by the invention provides a widely applicable preparation method for synthesis of the compounds.

Method for synthesizing phosphorus-oxychloride-promoted amide compound

The invention relates to a method for synthesizing a phosphorus-oxychloride-promoted amide compound. The synthesizing method includes the steps that carboxylic acid serves as one reactant, another reactant (N,N-dialkyl methanamide) serves as a solvent, one equivalent of phosphorus oxychloride is added, and the amide compound is prepared. The reaction substrates are low in price and easy to get, the nature is stable, toxicity is small, the reaction speed is high, conditions are moderate, and the reaction substrates can be widely applied to substrates with different functional groups. The efficiently-constructed amide compound is an important molecular skeleton for many medicines, bioactive molecules and natural products, and the synthesizing method is a widely-applicable preparing method for synthesizing the compound.

Beyond directed ortho metalation: Ru-catalyzed CAr-O activation/cross-coupling reaction by amide chelation

Disclosed is a new, catalytic, and general methodology for the chemical synthesis of biaryl, heterobiaryl, and polyaryl molecules by the cross-coupling of o-methoxybenzamides with aryl boroneopentylates. The reaction is based on the activation of the unreactive C-OMe bond by the proximate amide directing group using catalytic RuH2(CO)(PPh3)3 conditions. A one-step, base-free coupling process is thereby established that has the potential to supersede the useful two-step directed ortho metalation/cross- coupling reaction involving cryogenic temperature and strong base conditions. High regioselectivity, orthogonality with the Suzuki-Miyaura reaction, operational simplicity, minimum waste, and convenient scale-up make these reactions suitable for industrial applications.

ORGANIC COMPOUNDS

Compounds of the formula are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated. In addition, the compounds of the present invention may be employed to treat and/or prevent cancer (such as prostate or breast cancer), osteoporosis, neurodegenerative and infectious diseases, and diseases involving inflammation and the immune system.

Selective protein tyrosine phosphatatase inhibitors

Compounds of formula (I) or therapeutically acceptable salts thereof, are selective protein tyrosine kinase-B (PTP1B) inhibitors. Preparation of the compounds, compositions containing the compounds, and treatment of disorders using the compounds are disclosed.

Selective protein tyrosine phosphatatase inhibitors

Compounds of formula (I) or therapeutically acceptable salts thereof, are selective protein tyrosine kinase-B (PTP1B) inhibitors. Preparation of the compounds, compositions containing the compounds, and treatment of disorders using the compounds are disclosed.

A direct and mild conversion of tertiary aryl amides to methyl esters using trimethyloxonium tetrafluoroborate: A very useful complement to directed metalation reactions

The scope and generality of a direct process for the conversion of tertiary amides directly to methyl esters has been investigated. The process involves a two-step, one pot procedure in which a tertiary amide is first treated with trimethyloxonium tetrafluoroborate to generate an imidate intermediate which is then hydrolyzed, generally by the addition of saturated aqueous sodium bicarbonate solution. Although this process fails for aliphatic amides, very good yields are realized for a variety of amides derived from aromatic carboxylic acids. Steric hindrance at the N-alkyl group is well tolerated; thus N,N-dimethyl, -diethyl, and -diisopropyl amides can all be utilized successfully. (C) 2000 Elsevier Science Ltd.