276235-91-7

Usage

Uses

Used in Pharmaceutical Industry:
(5-FLUORO-1-BENZOFURAN-2-YL)METHANOL is used as a therapeutic agent for the treatment of neurodegenerative diseases, particularly Alzheimer's. Its application is based on its ability to inhibit the formation of Aβ fibrils, which are a key pathological feature of these diseases. By preventing the aggregation of amyloid-beta peptides, (5-FLUORO-1-BENZOFURAN-2-YL)METHANOL may help slow down or halt the progression of neurodegenerative conditions.
Additionally, due to its chemical properties and potential for further modification, (5-FLUORO-1-BENZOFURAN-2-YL)METHANOL could be utilized as a starting material or intermediate in the synthesis of other bioactive compounds with various applications in the pharmaceutical industry.

Upstream product

• 93849-31-1 ethyl 5-fluoro-1H-benzofuran-2-carboxylate 
• 849236-64-2 methyl 5-fluorobenzofuran-2-carboxylate 
• 371-41-5 4-Fluorophenol 
• 140382-35-0 5-fluorobenzofuran-2-carboxaldehyde 
• 347-54-6 5-fluoro-2-hydroxybenzaldehyde 

Downstream Products

• 140382-35-0 5-fluorobenzofuran-2-carboxaldehyde 

Relevant academic research and scientific papers

COMPOUND FOR INHIBITING PGE2/EP4 SIGNALING TRANSDUCTION INHIBITING, PREPARATION METHOD THEREFOR, AND MEDICAL USES THEREOF

A compound of formula (I), a preparation method therefor, a pharmaceutical composition containing a derivative thereof, and the therapeutic uses thereof, especially inhibiting PGE2/EP4 signalling transduction and the uses thereof for treating cancer, acute or chronic pain, migraine, osteoarthritis, rheumatoid arthritis, gout, bursitis, ankylosing spondylitis, primary dysmenorrhea, tumour or arteriosclerosis.

C- ARYL GLYCOSID DERIVATIVES, PHARMACEUTICAL COMPOSITION, PREPARATION PROCESS AND USES THEREOF

This invention relates to a kind of C-aryl glycoside derivatives, its pharmaceutical compositions, preparation methods, and uses thereof. The preparation method comprises: method 1: in a solvent, deprotecting the acetyl protecting groups of compound 1-f in the presence of a base; method 2: 1) compound 2-g reacts with via Mitsunobu reaction; 2) deprotecting the acetyl protecting groups of compound 2-f obtained from step 1; method 3: 1) compound 2-g reacts with via nucleophilic substitution reaction; 2) deprotecting the acetyl protecting groups of compound 3-f obtained from step 1. The pharmaceutical composition comprises a kind of C-aryl glycoside derivatives; it's pharmaceutically acceptable salts and/or prodrugs thereof and excipient thereof. This invention further relates to a kind of C-aryl glycoside derivatives, it's pharmaceutically acceptable salts or pharmaceutical compositions thereof for the use in preparation of a SGLT inhibitor. The C-aryl glycoside derivatives of this invention provides a new direction for the study of SGLT inhibitors.

2'-carbonyl-3-bromo-spiro[benzofuran-2,4'-oxazolidine] compounds and preparation method thereof

The invention discloses 2'-carbonyl-3-bromo-spiro[benzofuran-2, 4'-oxazolidine] compounds and a preparation method thereof. The 2'-carbonyl-3-bromo-spiro[benzofuran-2,4'-oxazolidine] compounds are photoactive compounds shown in the structural formula II. The 2'-carbonyl-3-bromo-spiro[benzofuran-2,4'-oxazolidine] compounds are photoactive spiro compounds, photoactive chiral spiro compounds with multiple functional groups substituted, such as photoactive chiral spiro compounds with azido groups, hydroxyl groups, allyl groups and anisole groups substituted, can be obtained through substitution reactions of bromine atoms at site 3 under different reaction conditions. Therefore, different kinds of other photoactive chiral spiro compounds are prepared by using the substitution reactions of bromine atoms, the range of the compounds is enlarged, and the potential application value is great.

Chromium-Catalyzed Asymmetric Dearomatization Addition Reactions of Halomethyl Heteroarenes

The first asymmetric dearomatization addition reaction of halomethyl arenes including benzofuran and benzothiophene was enabled by chromium catalysis. A variety of aldehydes served as suitable electrophiles under mild reaction conditions. Molecular complexities are quickly increased in a highly diastereo- and enantioselective manner.

SPIRO-OXADIAZOLINE COMPOUNDS AS AGONISTS OF α-7-NICOTINIC ACETYLCHOLINE RECEPTORS

The present invention relates to novel spiro-oxadiazoline compounds that are suitable as agonists or partial agonists of a7-nAChR, and pharmaceutical compositions of the same, methods of preparing these compounds and compositions, and the use of these compounds and compositions in methods of maintaining, treating and/or improving cognitive function. In particular, methods of administering a spiro-oxadiazoline cx7-nAChR agonist or partial agonist, to a patient in need thereof, for example a patient with a cognitive deficiency and/or a desire to enhance cognitive function, that may derive a benefit therefrom.

TREATMENT OR PROPHYLAXIS OF PROLIFERATIVE CONDITIONS

The invention relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. The invention also provides pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. The invention also provides methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1 B1 and allelic variants thereof. The invention also provides a method for determining the efficacy of a compound of the invention in treating cancer.

Aminostyrylbenzofuran derivatives as potent inhibitors for Aβ fibril formation

The synthesis of a novel series of aminostyrylbenzofuran derivatives 1a-w and their inhibitory activities for Aβ fibril formation were described. All the synthesized compounds were evaluated by thioflavin T (ThT) assay and displayed potent inhibitory activities for Aβ fibril formation. Among them, compounds 1i and 1q exhibited excellent inhibitory activities (IC50 = 0.07 and 0.08 μM, respectively) than those of Curcumin (IC50 = 0.80 μM) and IMSB (IC50 = 8.00 μM) as reference compounds. Both compounds were selected as promising candidates for further biological evaluation.