588703-29-1

Usage

Uses

Used in Pharmaceutical Research:
Methyl benzofuran-6-carboxylate is used as a versatile building block for the development of anti-cancer and anti-inflammatory drugs. Its unique structure and reactivity contribute to the creation of new molecules with potential therapeutic applications.
Used in Organic Synthesis:
Methyl benzofuran-6-carboxylate is utilized as a key intermediate in the synthesis of complex organic molecules, facilitating the development of novel chemical entities with diverse applications.
Used in Fragrance and Flavoring Industry:
Methyl benzofuran-6-carboxylate is employed as a component in the production of fragrances and flavorings, leveraging its unique chemical properties to create distinct scents and tastes.

Upstream product

• 67-56-1 methanol 
• 201230-82-2 carbon monoxide 
• 227752-25-2 trifluoromethanesulfonic acid benzofuran-6-yl ester 
• 478169-68-5 methyl 3-hydroxy-4-[(trimethylsilyl)ethynyl]benzoate 
• 13196-11-7 6-hydroxybenzofuran 
• 6272-26-0 6-hydroxybenzofuran-3-one 
• 299912-77-9 6-(tert-butyl-dimethylsilanyloxy)-[2H]-benzofuran-3-one 
• 616-38-6 carbonic acid dimethyl ester 
• 128851-73-0 6-bromo-benzofuran 
• 77095-51-3 benzofuran-6-carboxylic acid 
• 74-88-4 methyl iodide 
• 58123-77-6 3-hydroxy-4-iodobenzoic acid 
• 619-12-5 4-formyl-3-hydroxybenzoic acid 
• 99-06-9 3-Carboxyphenol 

Downstream Products

• 1194550-67-8 ((S)-benzyl 2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-methylsulfonyl)phenyl)propanoate 
• 1025967-78-5 (S)-2-(2-(benzofuran-6-carbonyl)-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carboxamido)-3-(3-(methylsulfonyl)phenyl)propanoic acid 
• 1083168-69-7 (2,3-dihydrobenzofuran-6-yl)methanol 
• 1056942-24-5 1-benzofuran-6-ylmethanol 
• 77095-51-3 benzofuran-6-carboxylic acid 

Relevant academic research and scientific papers

GLUE DEGRADERS AND METHODS OF USE THEREOF

Described herein are glue degrader compounds, their various targets, their preparation, pharmaceutical compositions comprising them, and their use in the treatment or prevention of conditions, diseases, and disorders mediated by various target proteins.

Method for preparing benzo oxygen-containing aliphatic heterocyclic derivative

The invention relates to a method for preparing a benzo oxygen-containing aliphatic heterocyclic derivative, which specifically comprises the following steps: (1) carrying out nitration reaction on acompound shown as a formula I-1 to obtain a compound shown as a formula I-2; (2) carrying out reduction reaction on the compound shown in the formula I-2 to obtain a compound shown in a formula I-3; (3) performing halogenation reaction on the compound shown in the formula I-3 to obtain a compound shown in a formula I-4; (4) carrying out diazotization reaction on the compound shown as the formula I-4, and further reacting the obtained product with a halogenated metal salt to generate a compound shown as a formula I;.

Preparation method of benzofuran derivative

The invention discloses a preparation method for synthesizing a benzofuran derivative. The specific implementation method is as shown in the specification. The method has novel synthetic route, simpleand convenient operation, high yield, and good safety, and is suitable for industrial production. A novel synthetic method of an intermediate VI is also designed, a Wittig reaction is carried out, and then ring-closing is carried out to obtain a benzofuran ring.

Synthesis method of lifitegrast intermediate

The invention provides a preparation method of a lifitegrast intermediate I. The method comprises steps as follows: 6-bromobenzo[b]furan is taken as a starting raw material and subjected to a halogen-lithium exchange reaction under the action of n-butyllithium, a product is subjected to a reaction with dimethyl carbonate, methyl benzofuran-6-carboxylate is prepared and hydrolyzed, and the lifitegrast intermediate I is obtained. The raw materials are cheap and easily available, few reaction by-products are produced, yield and purity of a final product are high, meanwhile, the step (1) an the step (2) can be subjected to the one-pot reaction, so that steps of the reaction are simplified, furthermore, the reaction conditions are mild, the product does not need separation on columns, and industrialization is easy to realize.

LFA-1 INHIBITOR AND POLYMORPH THEREOF

Methods of preparation and purification of a compound, intermediates thereof, a polymorph thereof, and related compounds are disclosed. Formulations and uses thereof in the treatment of LFA -1 mediated diseases are also disclosed.

Discovery and development of potent LFA-1/ICAM-1 antagonist SAR 1118 as an ophthalmic solution for treating dry eye

LFA-1/ICAM-1 interaction is essential in support of inflammatory and specific T-cell regulated immune responses by mediating cell adhesion, leukocyte extravasation, migration, antigen presentation, formation of immunological synapse, and augmentation of T-cell receptor signaling. The increase of ICAM-1 expression levels in conjunctival epithelial cells and acinar cells was observed in animal models and patients diagnosed with dry eye. Therefore, it has been hypothesized that small molecule LFA-1/ICAM-1 antagonists could be an effective topical treatment for dry eye. In this letter, we describe the discovery of a potent tetrahydroisoquinoline (THIQ)-derived LFA-1/ICAM-1 antagonist (SAR 1118) and its development as an ophthalmic solution for treating dry eye.

MODULATORS OF CFTR

Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette ("ABC") transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator ("CFTR"). The present invention also relates to methods of treating CFTR mediated diseases using compounds of the present invention.

Discovery of N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5- carboxamide, an agonist of the α7 nicotinic acetylcholine receptor, for the potential treatment of cognitive deficits in schizophrenia: Synthesis and structure-activity relationship

N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide (14, PHA-543,613), a novel agonist of the α7 neuronal nicotinic acetylcholine receptor (α7 nAChR), has been identified as a potential treatment of cognitive deficits in schizophrenia. Compound 14 is a potent and selective a7 nAChR agonist with an excellent in vitro profile. The compound is characterized by rapid brain penetration and high oral bioavailability in rat and demonstrates in vivo efficacy in auditory sensory gating and, in an in vivo model to assess cognitive performance, novel object recognition.

MODULATORS OF CELLULAR ADHESION

The present invention provides compounds having formula (I): and pharmaceutically acceptable derivatives thereof, wherein R1-R4, n, p, A, B, D, E, L and AR1 are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of disorders mediated by the CD11/CD18 family of cellular adhesion molecules (e.g., LFA-1).

Azabicyclic compounds for the treatment of disease

The invention provides compounds of Formula I: 1wherein Azabicyclo is 2These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals in which α7 is known to be involved.