84400-98-6

Usage

Uses

Used in Medicinal Chemistry:
Furo[2,3-c]pyridin-7(6H)-one is utilized as a key intermediate in the synthesis of various pharmaceutical compounds due to its unique fused-ring structure and potential biological activities.
Used in Drug Discovery:
Furo[2,3-c]pyridin-7(6H)-one is employed as a lead molecule in drug discovery for its potential therapeutic properties, such as anti-inflammatory, anti-cancer, and anti-microbial effects, which are being studied for the development of new medications.
Used in Organic Synthesis:
Furo[2,3-c]pyridin-7(6H)-one is used as a building block in organic synthesis for creating complex molecular structures that can be further modified for specific applications in chemical research and pharmaceutical development.
Used in Pharmaceutical Compounds:
Furo[2,3-c]pyridin-7(6H)-one is used as an active pharmaceutical ingredient in the development of new drugs that target a range of diseases and conditions, leveraging its biological activities for therapeutic benefits.

InChI:InChI=1/C7H5NO2/c9-7-6-5(1-3-8-7)2-4-10-6/h1-4H,(H,8,9)

Upstream product

• 541-41-3 chloroformic acid ethyl ester 
• 39244-10-5 (E)-3-furan-3-yl-acrylic acid 
• 39244-10-5 3-(furan-3-yl)prop-2-enoic acid 
• 84400-97-5 3-(furan-3-yl)prop-2-enoylazide 

Downstream Products

• 1140240-20-5 furo[2,3-c]pyridine-7-ylamine 
• 1326714-64-0 4-iodofuro[2,3-c]pyridin-7-ylamine 
• 1326714-70-8 2-{3,5-bis(trifluoromethyl)phenyl}-7-chlorofuro[2,3-c]pyridine 
• 1326714-71-9 2-{(3,5-bistrifluoromethyl)phenyl}furo[2,3-c]pyridin-7-ylamine 
• 1326714-72-0 2-{3,5-bistrifluoromethylphenyl}-4-bromofuro[2,3-c]pyridin-7-ylamine 
• 1326714-73-1 tert-butyl 4-(4-{7-amino-2-[3,5-bis(trifluoromethyl)phenyl]furo[2,3-c]pyridin-4-yl}-1H-pyrazol-1-yl)piperidine-1-carboxylate 

Relevant academic research and scientific papers

HETEROCYCLIC SULFONAMIDE DERIVATIVE AND MEDICINE COMPRISING SAME

The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the DESCRIPTION, or a pharmaceutically acceptable salt thereof. The compound has a superior TRPA1 antagonist activity, and can provide a medicament useful for the prophylaxis or treatment of diseases involving TRPA1 antagonist and TRPA1.

NOVEL COMPOUNDS AS REARRANGED DURING TRANSFECTION (RET) INHIBITORS

This invention relates to novel compounds which are inhibitors of the Rearranged during Transfection (RET) kinase, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination, for the normalization of gastrointestinal sensitivity, motility and/or secretion and/or abdominal disorders or diseases and/or treatment related to diseases related to RET dysfunction or where modulation of RET activity may have therapeutic benefit including but not limited to all classifications of irritable bowel syndrome (IBS) including diarrhea-predominant, constipation-predominant or alternating stool pattern, functional bloating, functional constipation, functional diarrhea, unspecified functional bowel disorder, functional abdominal pain syndrome, chronic idiopathic constipation, functional esophageal disorders, functional gastroduodenal disorders, functional anorectal pain, inflammatory bowel disease, proliferative diseases such as non-small cell lung cancer, hepatocellular carcinoma, colorectal cancer, medullary thyroid cancer, follicular thyroid cancer, anaplastic thyroid cancer, papillary thyroid cancer, brain tumors, peritoneal cavity cancer, solid tumors, other lung cancer, head and neck cancer, gliomas, neuroblastomas, Von Hippel-Lindau Syndrome and kidney tumors, breast cancer, fallopian tube cancer, ovarian cancer, transitional cell cancer, prostate cancer, cancer of the esophagus and gastroesophageal junction, biliary cancer, adenocarcinoma, and any malignancy with increased RET kinase activity.

Discovery and optimization of 7-aminofuro[2,3-c]pyridine inhibitors of TAK1

The discovery and potency optimization of a series of 7-aminofuro[2,3-c] pyridine inhibitors of TAK1 is described. Micromolar hits taken from high-throughput screening were optimized for biochemical and cellular mechanistic potency to ～10 nM, as exemplified by compound 12az. Application of structure-based drug design aided by co-crystal structures of TAK1 with inhibitors significantly shortened the number of iterations required for the optimization.

7-AMINOFUROPYRIDINE DERIVATIVES

Compounds of Formula 1, as shown below and defined herein: pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven at least in part by TAK1 or for which an appropriate TAK1 inhibitor is effective. This Abstract is not limiting of the invention.

Synthesis of highly substituted cyclobutane fused-ring systems from n-vinyl β-lactams through a one-pot domino process

In this contribution, aminocyclobutanes, as well as eight-membered enamide rings, have been made from N-vinyl β-lactams. The eightmembered products have been formed by a [3,3]-sigmatropic rearrangement, whereas the aminocyclobutanes have been derived from a domino [3,3]-rearrangement/6π- electrocyclisation process. The aminocyclobutanes have been obtained in a highly diastereoselective fashion. The cyclobutane ring system tolerates fusion even if adjacent quaternary centres are present. Systems containing up to four fused rings are readily accessible. The reaction profile has been investigated by using Gaussian 03. This study suggests that two reaction pathways for aminocyclobutane formation are possible. In one pathway the [3,3]-sigmatropic rearrangement is the rate-limiting step and in the second pathway the electrocyclisation is rate limiting. Taken together, these reactions should facilitate the construction of fused heterocycles.

Synthesis of aminocyclobutanes through ring expansion of N-vinyl-β-lactams

Both eight-membered enamide rings and fused [4.2.0]aminocyclobutane- containing δ-lactams can be accessed from N-vinyl-β-lactams. The eight-membered rings are made through a [3,3] sigmatropic rearrangement. At elevated temperature, the eight-membered lact

Design and synthesis of piperazinylpyridine derivatives as novel 5-HT 1A agonists/5-HT3 antagonists for the treatment of irritable bowel syndrome (IBS)

We have prepared a series of piperazinylpyridine derivatives for the treatment of irritable bowel syndrome (IBS). These compounds, which were designed by pharmacophore analysis, bind to both serotonin subtype 1A (5-HT 1A) and subtype 3 (5-HT3) receptors. The nitrogen atom of the isoquinoline, a methoxy group and piper-azine were essential to the pharmacophore for binding to these receptors. We also synthesized furo- and thienopyridine derivatives according to structure-activity relationship analyses. Compound 17c (TZB-20810) had high affinities to these receptors and exhibited 5-HT1A agonistic activity and 5-HT3 antagonistic activity concurrently, and is a promising drug for further development in the treatment of IBS.

PYRIMIDINE DERIVATIVE

This invention provides pyrimidine derivatives represented by a formula, in the formula, ring A stands for carbocyclic group or heterocyclic group, X 1 stands for hydrogen, lower alkyl, amino, etc., X 2 stands for hydrogen or lower alkyl, Y stands for a direct bond or sulfur or nitrogen, n stands for an integer of 0 - 4, and Ar stands for a group of the following formula, or a salt thereof, which concurrently exhibit 5-HT 1A agonistic activity and 5-HT 3 antagonistic activity and are useful for therapy and treatments of diseases such as IBS. The invention furthermore provides a therapeutic method of IBS, characterized by having 5-HT 1A agonistic activity and 5-HT 3 antagonistic activity work simultaneously and cooperatively in vivo, which comprises either administering 5-HT 3 antagonistic agent which concurrently exhibits 5-HT 1A agonistic activity, or administering 5-HT 1A agonistic agent and 5-HT 3 antagonistic agent simultaneously, in sequence or at an interval.

Furopyridines. I. Synthesis of Furopyridine

The parent framework of furopyridine has been synthesized. 3-Furoic acid chloride (2) was reduced with bis(triphenylphosphine) copper(I) tetrahydroborate to afford 3-furaldehyde (3) which was condensed with malonic acid to give β-(3-furyl)acrylic acid (4).The acrylic acid 4 was converted to the acid azide (5), which in turn was cyclized to give furopyridin-7(6H)-one (6) by heating at 180 deg in diphenylmethane.The pyridone 6 was chlorinated with phosphorus oxychloride, followed by reduction with zinc and acetic acid to give furopyridine (8).