6965-69-1

Usage

Uses

Used in Pharmaceutical Industry:
2-FORMYL-4-NITROPHENOXYACETIC ACID is used as a precursor in the synthesis of various pharmaceuticals for its ability to be modified and transformed into different active ingredients. This allows for the development of new drugs and therapeutic agents to address a range of health conditions.
Used in Agrochemical Industry:
In agriculture, 2-FORMYL-4-NITROPHENOXYACETIC ACID is utilized as a starting material for the production of agrochemicals. Its versatility in chemical synthesis enables the creation of effective compounds for pest control, crop protection, and other agricultural applications, thereby enhancing agricultural productivity and crop yields.

InChI:InChI=1/C9H7NO6/c11-4-6-3-7(10(14)15)1-2-8(6)16-5-9(12)13/h1-4H,5H2,(H,12,13)

Upstream product

• 6280-80-4 2-Formylphenoxyacetic acid 
• 97-51-8 5-Nitrosalicylaldehyde 
• 79-11-8 chloroacetic acid 
• 90-02-8 salicylaldehyde 
• 119197-73-8 2-Formyl-4-nitro-phenoxyessigsaeure-methylester-dimethylacetal 
• 24582-00-1 (2-formyl-4-nitrophenoxy)acetic acid methyl ester 

Downstream Products

• 24589-96-6 [(α-hydroxy-4-nitro-o-tolyl)oxy]-acetic acid 
• 162509-45-7 (E)-(2-hydroxyiminomethyl-4-nitrophenoxy)acetic acid 
• 24582-00-1 (2-formyl-4-nitrophenoxy)acetic acid methyl ester 
• 1156670-01-7 5-nitro-2-(2-oxo-2-pyrrolidin-1-ylethoxy)benzaldehyde 
• 1354567-02-4 2-{2-[(allylmethylamino)methyl]-4-nitrophenoxy}-1-pyrrolidin-1-ylethanone 
• 1354567-45-5 2-{2-[(allylmethylamino)methyl]-4-aminophenoxy}-1-pyrrolidin-1-ylethanone 
• 1354567-66-0 2-{2-[(allylmethylamino)methyl]-4-[4-(3-but-3-enyloxyphenyl)pyrimidin-2-ylamino]phenoxy}-1-pyrrolidin-1-ylethanone 
• 267644-49-5 5-nitro-1-benzofuran-2-carboxamide 
• 183288-46-2 5-(1-piperazinyl)benzofuran-2-carboxamide 
• 163521-12-8 vilazodone 
• 10242-12-3 5-nitrobenzofuran-2-carboxylic acid 
• 162509-46-8 (E)-2-methoxyiminomethyl-4-nitro-phenoxyacetic acid 
• 18761-31-4 5-nitrobenzofuran 
• 227286-81-9 (E)-(4-amino-2-hydroxyiminomethylhenoxy)acetic acid 

Relevant academic research and scientific papers

Design, synthesis, and biological evaluation of thiazolidine-2,4-dione conjugates as PPAR-γ agonists

A library of synthesized conjugates of phenoxy acetic acid and thiazolidinedione 5a-m showed potent peroxisome proliferator activated receptor-γ (PPAR-γ) transactivation as well as significant blood glucose lowering effect comparable to the standard drugs pioglitazone and rosiglitazone. Most of the compounds showed higher docking scores than the standard drug rosiglitazone in the molecular docking study. Compounds 5l and 5m exhibited PPAR-γ transactivation of 54.21 and 55.41%, respectively, in comparison to the standard drugs pioglitazone and rosiglitazone, which showed 65.94 and 82.21% activation, respectively. Compounds 5l and 5m significantly lowered the blood glucose level of STZ-induced diabetic rats. Compounds 5l and 5m lowered the AST, ALT, and ALP levels more than the standard drug pioglitazone. PPAR-γ gene expression was significantly increased by compound 5m (2.00-fold) in comparison to the standard drugs pioglitazone (1.5-fold) and rosiglitazone (1.0-fold). Compounds 5l and 5m did not cause any damage to the liver and could be considered as promising candidates for the development of new antidiabetic agents.

POLYMORPHIC FORM OF 5-(4-[4-(5-CYANO-1H-INDOL-3-YL) BUTYL] PIPERAZIN-1-YL) BENZOFURAN-2-CARBOXAMIDE AND PROCESS FOR PREPARING THEREOF

The present invention provides a solid state Form-Z of 5-(4-[4-(5-cyano-1H-indol-3-yl)butyl]piperazin-1-yl)benzofuran-2-carboxamide. The present invention also provides a process for preparing Form-Z of 5-(4-[4-(5-cyano-1H-indol-3-yl)butyl]piperazin-1-yl)benzofuran-2-carboxamide comprising the steps of i) reacting solid state form of 5-(1-piperazinyl)benzofuran-2-carboxamide or its salts with 3-(4-chlorobutyl)-1H-indole-5-carbonitrile an organic solvent in presence of a base to obtain crude vilazodone free base; ii) purifying the crude vilazodone free base of step (i) in an organic solvent; iii) treating the purified vilazodone free base of step (ii) with an organic solvent to obtain solid state form-Z of vilazodone. The present invention further provides a pharmaceutical composition comprising a therapeutically effective amount of an amorphous form of vilazodone hydrochloride and use of solid state Form-Z of vilazodone for the treatment of major depressive disorders.

POLYMORPHIC FORM OF 5-(4-[4-(5-CYANO-1H-INDOL-3- YL)BUTYL]PIPERAZIN-1-YL) BENZOFURAN-2-CARBOXAMIDE

The present invention relates to a process for the preparation of 5-(4-[4-(5- cyano- 1 H-indol-3 -yl)butyl] piperazin- 1 -yl)benzofuran-2-carboxamide of Formula (1) or its pharmaceutically acceptable salt, solvates or hydrates thereof. In particular, the present invention provides a novel intermediate compound, 5-(4-substitutedpiperazin- 1-yl)benzofuran-2-carboxamide of Formula (X). The present invention further provides solid state form of 5-(4-[4-(5-cyano-1H-indol-3- yl) butyl]piperazin-1-yl)benzofuran-2-carboxamide of Formula (1) and process for its preparation.

Discovery of kinase spectrum selective macrocycle (16E)-14-methyl-20-oxa-5, 7,14,26-tetraazatetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8(27) ,9,11,16,21,23-decaene (SB1317/TG02), a potent inhibitor of cyclin dependent kinases (CDKs), Janus kinase 2 (JAK2), and Fms-like tyrosine kinase-3 (FLT3) for the treatment of cancer

Herein, we describe the design, synthesis, and SAR of a series of unique small molecule macrocycles that show spectrum selective kinase inhibition of CDKs, JAK2, and FLT3. The most promising leads were assessed in vitro for their inhibition of cancer cell proliferation, solubility, CYP450 inhibition, and microsomal stability. This screening cascade revealed 26h as a preferred compound with target IC50 of 13, 73, and 56 nM for CDK2, JAK2 and FLT3, respectively. Pharmacokinetic (PK) studies of 26h in preclinical species showed good oral exposures. Oral efficacy was observed in colon (HCT-116) and lymphoma (Ramos) xenograft studies, in line with the observed PK/PD correlation. 26h (SB1317/TG02) was progressed into development in 2010 and is currently undergoing phase 1 clinical trials in advanced leukemias and multiple myeloma.

SUBSTITUTED TRIAZOLE DERIVATIVES AS OXYTOCIN ANTAGONISTS

The present invention relates to a class of substituted triazoles of formula (I) with activity as oxytocin antagonists, uses thereof, processes for the preparation thereof and compositions containing said inhibitors. These inhibitors have utility in a variety of therapeutic areas including sexual dysfunction, particularly premature ejaculation (P.E.).

Synthesis and activity of cephalosporins containing an oxyiminomethylene functionality in the ortho-position of a phenyl- or phenoxyacetic acid C-7 side chain substituent

A new series of cephalosporins having in the C-7 side chain a phenyl- or a phenoxyacetamido group bearing an oxyiminomethyl function in the ortho-position of the aromatic ring was prepared. Their in vitro activity was tested against both Gram+ and Gram- s