1878-88-2

Usage

Chemical Properties

yellow-beige crystalline powder

Upstream product

• 554-84-7 meta-nitrophenol 
• 105-36-2 ethyl bromoacetate 
• 79-08-3 bromoacetic acid 
• 79-14-1 glycolic Acid 
• 645-00-1 m-iodonitrobenzene 
• 5544-77-4 2-(3-nitrophenoxy)-acetic acid ethyl ester 
• 3019-85-0 sodium 3-nitrophenoxide 
• 40257-02-1 3-nitrophenoxyacetyl chloride 
• 20916-36-3 (3-nitro-phenoxy)-acetic acid anilide 
• 3926-62-3 sodium monochloroacetic acid 
• 138563-69-6 tert-butyl 2-(3-nitrophenoxy)acetate 
• 79-11-8 chloroacetic acid 
• 81720-19-6 1-methoxycarbonylmethyloxy-3-nitrobenzene 

Downstream Products

• 1093409-09-6 KNI-10255 
• 1107603-67-7 C₂₃H₃₂N₂O₇ 
• 1107603-68-8 C₂₃H₃₂N₂O₇ 
• 916438-53-4 N-methyl-3-nitrophenoxyacetamide 
• 847606-70-6 N-(4-chloro-3-trifluoromethylphenyl)-2-[3-(4-trimethylsilanyl-[1,2,3]triazol-1-yl)-phenoxy]-acetamide 
• 847606-74-0 N-[4-chloro-3-(trifluoromethyl)phenyl]-2-{[3-(5-methyl-1H-tetrazol-1-yl)phenyl]oxy}acetamide 
• 506433-09-6 N-[4-chloro-3-(trifluoromethyl)phenyl]-2-{[3-(1H-tetrazol-1-yl)-phenyl]oxy}-acetamide 
• 847606-67-1 N-[4-chloro-3-(trifluoromethyl)phenyl]-2-{[3-(1H-1,2,3-triazol-1-yl)phenyl]oxy}acetamide 
• 847606-78-4 N-[4-chloro-3-(trifluoromethyl)phenyl]-2-{[4-(1,2,4-triazol-4-yl)phenyl]oxy}acetamide 
• 847606-69-3 [3-(4-trimethylsilanyl-[1,2,3]triazol-1-yl)-phenoxy]-acetic acid 
• 847606-75-1 [3-(5-methyl-tetrazol-1-yl)-phenoxy]-acetic acid 
• 462067-31-8 3-tetrazol-1-ylphenoxyacetic acid 
• 847606-68-2 (3-azidophenoxy)-acetic acid 
• 916737-63-8 3-(3-methyl-1,2,4-oxadiazol-5-yl)methyloxyaniline 

Relevant academic research and scientific papers

Adamantyl quinazoline compound, composition and application of adamantyl quinazoline compound and composition

The invention discloses an adamantyl quinazoline compound, a composition and application of the adamantyl quinazoline compound and the composition. The compound shown in a formula (I) and all possible isomers or pharmaceutically acceptable salts or hydrates or compositions are used to treat diseases caused by EGFR (Epidermal Growth Factor Receptor) tyrosine kinase, and are particularly used to treat non-small cell lung cancer, small cell lung cancer, squamous-cell carcinoma, breast cancer and gastric carcinoma.

2,4-Pyrimidinediamine Compounds and Their Uses

The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.

METHOD AND DEVICE FOR ADMINISTERING XINAFOATE SALT OF N4-(2,2-DIFLUORO-4H-BENZO [1,4]OXAZIN-3-ONE)-6-YL]-5-FLUORO-N2-[3- (METHYLAMINOCARBONYLMETHYLENEOXY) PHENYL]2,4-PYRIMIDINEDIAMINE

Disclosed embodiments concern a device for administering a xinafoate salt of N4-[(2,2-difluoro-4H-benzo[1,4]oxazin-3-one)-6-yl]-5-fluoro-N2-[3-(methylaminocarbonylmethyleneoxy)phenyl]-2,4-pyrimidinediamine, or compositions thereof, and a method for making and using the device. Particular disclosed embodiments concern formulating the xinafoate salt for administration via the device.

Copper(II)-catalyzed hydroxylation of aryl halides using glycolic acid as a ligand

Copper(II)-catalyzed hydroxylation of aryl halides has been developed to afford functionalized phenols. The protocol utilizes the reagent combination of Cu(OH)2, glycolic acid, and NaOH in aqueous DMSO, all of which are cheap, readily available, and easily removable after the reaction. A broad range of aryl iodides and activated aryl bromides were transformed into the corresponding phenols in excellent yields. Moreover, it has been shown that C-O(alkyl)-coupled product, instead of phenol, can be predominantly formed under similar reaction conditions.

Aza-Michael addition of acrylonitrile with 2-aryloxymethylbenzimidazole derivatives under microwave irradiation

A simple, rapid, and highly efficient method has been developed for the aza-Michael addition of acrylonitrile to 2-aryl-oxymethylbenzimidazole derivatives in the presence of anhydrous potassium carbonate under microwave irradiation. A series novel of 1-cyanoethyl-2-aryloxymethylbenzimidazole derivatives have been prepared and characterised by 1H NMR, 13C NMR, IR spectra and elemental analysis.

HETEROARYL COMPOUNDS AND USES THEREOF

The present invention provides inhibitors of protein kinases of formula I-a and I-b, pharmaceutically acceptable compositions thereof, and methods of using the same.

Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin

Plasmepsin (Plm) is a potential target for new antimalarial drugs, but most reported Plm inhibitors have relatively low antimalarial activities. We synthesized a series of dipeptide-type HIV protease inhibitors, which contain an allophenylnorstatine-dimethylthioproline scaffold to exhibit potent inhibitory activities against Plm II. Their activities against Plasmodium falciparum in the infected erythrocyte assay were largely different from those against the target enzyme. To improve the antimalarial activity of peptidomimetic Plm inhibitors, we attached substituents on a structure of the highly potent Plm inhibitor KNI-10006. Among the derivatives, we identified alkylamino compounds such as 44 (KNI-10283) and 47 (KNI-10538) with more than 15-fold enhanced antimalarial activity, to the sub-micromolar level, maintaining their potent Plm II inhibitory activity and low cytotoxicity. These results suggest that auxiliary substituents on a specific basic group contribute to deliver the inhibitors to the target Plm.

Synthesis and anti-inflammatory activity of 2-aryloxy methyl oxazolines

A series of potential biologically active 2-aryloxy methyl oxazolines 3a-n have been synthesized from substituted hydroxybenzenes 1a-n with good chemical yield. The compounds 3a-n were screened for their anti-inflammatory, ulcerogenic, cyclooxygenase activities and also for their acute toxicity. The potency of the compounds was compared with that of the standard drugs, aspirin and phenyl butazone. The outcome indicates that compounds 3b (48.2%), 3h (48.5%) and 3l (46.5%) offered significant anti-inflammatory activity with low ulcerogenic activity than the standard drugs.

A rapid and high-yield synthesis of aryloxyacetic acid in one pot under microwave irradiation and phase transfer catalysis conditions

A series of aryloxyacetic acid 3a-h has been synthesized in one pot under microwave irradiation and phase transfer catalysis conditions. By the optimization of the reaction condition, a rapid, high-yield and efficient method for the preparation of aryloxyacetic acid is reported.

A convenient preparation of N-alkyl and N-arylamines by smiles rearrangement - Synthesis of analogues of diclofenac

Smiles rearrangement of substituted aryloxyacetamides in which oxygen and nitrogen are separated by COCH2 group has been successful even when the aryloxy ring carries weak or no electron withdrawing group. Earlier reports of such reactions involved either strong electron withdrawing groups or a special catalyst. The diphenylamines thus obtained gave analogues of diclofenac in only one case.