7356-11-8

Usage

Synthesis

Methyl 4-methyl-3-nitrobenzoate is synthesized by the following steps:Acid 33 (100 g, 0.552 mol) was dissolved in MeOH (1000 ml). Conc. ?H2SO4 (30 ml) was added cautiously to this solution. The mixture was ?refluxed for 8 hours. Solvent was distilled off. Ice-cold water was added ?to the residue. It was then extracted with EtOAc, washed with NaHCO3 solution, water, dried (anhydrous Na2SO4), filtered and concentrated in ?vacuo to furnish faint yellow a solid. (91.57 g).

Chemical Properties

White solid

Uses

Methyl 4-methyl-3-nitrobenzoate is used as pharmaceutical intermediate.

InChI:InChI=1/C9H9NO4/c1-6-3-4-7(9(11)14-2)5-8(6)10(12)13/h3-5H,1-2H3

Upstream product

• 67-56-1 methanol 
• 96-98-0 4-methyl-3-nitrobenzoic acid 
• 99-75-2 4-methyl-benzoic acid methyl ester 
• 7647-01-0 hydrogenchloride 
• 939-79-7 4-cyano-2-nitrotoluene 
• 77-78-1 dimethyl sulfate 
• 7697-37-2 nitric acid 
• 159583-78-5 methyl 4-<(phenylthio)methyl>-3-nitrobenzoate 

Downstream Products

• 88089-94-5 methyl 4-bromomethyl-3-nitrobenzoate 
• 104447-80-5 (E)-1-(dimethylamino)-2-[4-(methoxycarbonyl)-2-nitrophenyl]ethene 
• 170487-40-8 1H-indazole-6-carboxylic acid methyl ester 
• 1630015-59-6 3-phenyl-5-(6-indazolyl)-1,2,4-oxadiazole 
• 1630015-60-9 3-(3-methylphenyl)-5-(6-indazolyl)-1,2,4-oxadiazole 
• 1630015-61-0 3-(3-fluorophenyl)-5-(6-indazolyl)-1,2,4-oxadiazole 
• 832075-29-3 C₉H₁₂N₂O₂ 
• 1071679-94-1 3-isocyanato-4-methyl-benzoic acid methyl ester 
• 88072-09-7 3-(3-Bromo-propionylamino)-4-phenoxymethyl-benzoic acid methyl ester 
• 88072-19-9 3-(2-Oxo-azetidin-1-yl)-4-phenoxymethyl-benzoic acid methyl ester 
• 88072-27-9 3-(2-Oxo-azetidin-1-yl)-4-phenoxymethyl-benzoic acid 
• 88071-93-6 nitro-3 phenoxymethyl-4 benzoate de methyle 
• 88089-54-7 4-Bromomethyl-3-(2-oxo-azetidin-1-yl)-benzoic acid 
• 88071-97-0 amino-3 phenoxymethyl-4 benzoate de methyle 

Relevant academic research and scientific papers

Design, Synthesis, and in vitro Evaluation of P2X7 Antagonists

The P2X7 receptor is a promising target for the treatment of various diseases due to its significant role in inflammation and immune cell signaling. This work describes the design, synthesis, and in vitro evaluation of a series of novel derivatives bearing diverse scaffolds as potent P2X7 antagonists. Our approach was based on structural modifications of reported (adamantan-1-yl)methylbenzamides able to inhibit the receptor activation. The adamantane moieties and the amide bond were replaced, and the replacements were evaluated by a ligand-based pharmacophore model. The antagonistic potency of the synthesized analogues was assessed by two-electrode voltage clamp experiments, using Xenopus laevis oocytes that express the human P2X7 receptor. SAR studies suggested that the replacement of the adamantane ring by an aryl-cyclohexyl moiety afforded the most potent antagonists against the activation of the P2X7 cation channel, with analogue 2-chloro-N-[1-(3-(nitrooxymethyl)phenyl)cyclohexyl)methyl]benzamide (56) exhibiting the best potency with an IC50 value of 0.39 μΜ.

FUSED BICYCLIC COMPOUNDS AND USES THEREOF IN MEDICINE

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One-pot synthesis of novel 3,5-disubstituted-1,2,4-oxadiazoles from indazole carboxylic acid esters and amidoximes

An efficient and high-yielding one-pot synthesis of 3,5-disubstituted-1,2, 4-oxadiazoles from indazole carboxylic acid methyl esters and amidoximes is described. In this study a series of novel 3,5-disubstituted-1,2,4-oxadiazoles (3a-d), (4a-d), (5a-d), (6a-d), (7a-d) were synthesized using amidoximes 2a-d and indazole carboxylic acid esters (3-6).

GLUTAMATE DERIVATIVES OR SALTS THEREOF

Compounds having an excellent CaSR agonist activity are in demand. The invention provides glutamate derivatives or salts thereof, pharmaceutical compositions comprising the glutamate derivatives, preventive or therapeutic agents for diarrhea, hyperparathyroidism or peptic ulcer.

PROPHYLACTIC AGENT OR THERAPEUTIC AGENT FOR DIABETES OR OBESITY

A medicament having an excellent CaSR agonist action which enables the prevention or treatment of diabetes or obesity is provided by a composition comprising the compound represented by general formula (I) as defined, or a salt thereof.

SUBSTITUTED HETEROCYCLIC ACETAMIDES AS KAPPA OPIOID RECEPTOR (KOR) AGONISTS

The present invention relates to a series of substituted compounds having the general formula (I), including their ste reoisomers and/or their pharmaceutically acceptable salts, wherein R1, R2, R3. R4, R5, and R6 are as defined herein. This invention also relates to methods of making these compounds including intermediates. The compounds of this invention are effective at the kappa (κ) opioid receptor (KOR) site. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic pain, and associated disorders, particularly functioning peripherally at the CNS.

RING-FUSED COMPOUND

The present invention relates to a compound that has URAT1 inhibitory action, and a URAT1 inhibitor, a blood uric acid level-reducing agent and a pharmaceutical composition comprising the compound. More specifically, the present invention relates to a compound represented by Formula (I) below. [in the formula, R1 is -Q1-A1 and the like; ---- is a double bond or a single bond; when ---- is a double bond, W1 is a nitrogen atom or a group represented by the general formula: =C(Ra)-, and W2 is a nitrogen atom or a group represented by the general formula: =C(Rb) -; when ---- is a single bond, W1 is a group represented by the general formula: -C(Raa)(Rab)- or a group represented by the general formula: -(C=O) -, and W2 is a group represented by the general formula: C(Rba)(Rbb)-, a group represented by the general formula: - (C=O) - or a group represented by the general formula: -N(Rbc)-; W3, W4 and W5 are each independently a nitrogen atom or a methine group and the like that may have a substituent; X is a single bond, an oxygen atom and the like; Y is a single bond or (CRYiRYi')n; and Z is a hydroxyl group or COOR2 and the like.

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Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.

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Disclosed are compounds, compositions and methods for treatingFlaviviridae family virus infections.

BICYCLIC DERIVATIVES AS PPAR MODULATORS

The present invention is directed to compounds represented by the following structural formula, Formula (I), and stereoisomers, pharmaceutically acceptable salts, solvates and hydrates thereof, wherein: (a) R2 is selected from the group consisting of C0-C8 alkyl and C1-4- heteroalkyl; (b) X is selected from the group consisting of a single bond, O, S, S(O)2 and N; (c) U is an aliphatic linker wherein one carbon atom of the aliphatic linker is optionally replaced with O, NH or S, and wherein such aliphatic linker is optionally substituted with from one to four substituents each independently selected from R30; (d) Y is selected from the group consisting of C, O, S, NH and a single bond; and (e) E is C(R3)(R4)A or A.