299912-77-9

Usage

Uses

Used in Organic Synthesis:
6-((tert-butyldimethylsilyl)oxy)benzofuran-3(2H)-one is utilized as a protecting group for alcohols in organic synthesis. It facilitates selective manipulation of reactive functional groups within a molecule, which is crucial for the synthesis of complex organic compounds.
Used in Pharmaceutical Preparation:
6-((tert-butyldimethylsilyl)oxy)benzofuran-3(2H)-one plays a significant role in the preparation of various pharmaceuticals and bioactive compounds. Its ability to protect and selectively modify functional groups makes it an essential component in the development of new drugs.
Used in Materials Science:
6-((tert-butyldimethylsilyl)oxy)benzofuran-3(2H)-one also has potential applications in materials science. Its unique structure and properties can contribute to the development of new materials with specific characteristics for various uses.
Used as a Reagent in Organic Chemistry Reactions:
Furthermore, 6-((tert-butyldimethylsilyl)oxy)benzofuran-3(2H)-one serves as a reagent in a range of organic chemistry reactions. Its versatility allows it to participate in multiple reaction types, broadening its utility in chemical research and development.

Upstream product

• 288-32-4 1H-imidazole 
• 6272-26-0 6-hydroxybenzofuran-3-one 
• 18162-48-6 tert-butyldimethylsilyl chloride 

Downstream Products

• 227752-25-2 trifluoromethanesulfonic acid benzofuran-6-yl ester 
• 1083168-69-7 (2,3-dihydrobenzofuran-6-yl)methanol 
• 134937-20-5 2-(3,5-dimethoxyphenyl)-6-hydroxybenzofuran 
• 218444-39-4 2-[[3,5-dimethoxy-4-(3-methyl-2-butenyl)]phenyl]-6-(tert-butyldimethylsilanyloxy)benzofuran 
• 218444-38-3 2-(3,5-dimethoxyphenyl)-6-(tert-butyl-dimethylsilanyloxy)benzofuran 
• 56317-21-6 moracin M 
• 69120-07-6 moracin D 
• 936006-11-0 2-[3',5'-dihydroxy-4'-(3-methlbut-1-enyl)phenyl]-6-hydroxybenzofuran 
• 69120-06-5 moracin C 
• 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 
• 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 
• 588703-29-1 methyl benzofuran-6-carboxylate 
• 77095-51-3 benzofuran-6-carboxylic acid 
• 204452-96-0 (S)-3-Benzofuran-6-yl-3-[benzyl-((R)-1-phenyl-ethyl)-amino]-propionic acid ethyl ester 

Relevant academic research and scientific papers

PD-1/PD-L1 small-molecule inhibitor and preparation method and application thereof

The invention discloses a PD-1/PD-L1 small-molecule inhibitor and a preparation method and application thereof. Specifically, the invention discloses a compound with the structure shown in the formulaL, a stereoisomer or a tautomer thereof, or pharmaceutically acceptable salts or hydrates or solvates thereof, and please see the specification for specific definitions. The compound has excellent effects for restraining PD-1/PD-L1. Please see the specification for the formula.

Total synthesis of the 2-arylbenzo[b]furan-containing natural products from Artocarpus

In this study, 2-arylbenzo[b]furan-containing derivatives moracin C (1) and moracin M (4), the natural products from Artocarpus, have been synthesized in highest overall yield to date (1, 7 steps with an overall yield of 41.9%; 4, 6 steps with an overall yield of 56.3%), and we also report the first total synthesis of artoindonesianin B-1 (2), another member of this family, in the same route (8 steps with an overall yield of 11.3%). This discovery provides a concise route for preparing enough amounts of 1, 2, and 4 as well as 2-arylbenzo[b]furan-containing natural product-like analogs (71-74) to explore the biological potential.

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.

ANTIDIABETIC BICYCLIC COMPOUNDS

Tricyclic compounds containing a cyclopropyl carboxylic acid or carboxylic acid derivative (e.g. amide) fused to a bicyclic ring, including pharmaceutically acceptable salts and prodrugs thereof, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

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).

Nonpeptide alphavbeta3 antagonists. Part 11: discovery and preclinical evaluation of potent alphavbeta3 antagonists for the prevention and treatment of osteoporosis.

3-(S)-Pyrimidin-5-yl-9-(5,6,7,8-tetrahydro-[1,8]naphthyridin-2-yl)-nonanoic acid (5e) and 3-(S)-(methylpyrimidin-5-yl)-9-(5,6,7,8-tetrahydro-[1,8]naphthyridin-2-yl)-nonanoic acid (5f) were identified as potent and selective antagonists of the alpha(v)beta(3) receptor. These compounds have excellent in vitro profiles (IC(50) = 0.07 and 0.08 nM, respectively), significant unbound fractions in human plasma (6 and 4%), and good pharmacokinetics in rat, dog, and rhesus monkey. On the basis of the efficacy shown in an in vivo model of bone turnover following once-daily oral administration, these two compounds were selected for clinical development for the treatment of osteoporosis.

Novel benzofuran derivatives

The present invention provides novel benzofuran derivatives represented by the following formula (I) or salts thereof: wherein Py is a 2-, 3-, or 4-pyridyl group and R is a substituted or unsubstituted phenyl group or a substituted or unsubstituted aromatic heterocyclic group. The present invention also relates to inhibitors of steroid 17α-hydroxylase and/or steroid C17-20 lyase and pharmaceutical compositions containing a benzofuran derivative of the above formula (I), or the salt.

Syntheses of 5- and 6-[2,3]-dihydrobenzofuran β-amino acids

Efficient stereoselective syntheses of 5- and 6-[2,3]-dihydrobenzofuran β-amino acids are described. These 3-aryl β-amino acids are aspartic acid mimetics that are structurally related to known benzodioxole systems. In many cases, the benzodioxole can inhibit and induce cytochrome P-450; neither of these dihydrobenzofuran β-amino esters is a potent inhibitor of several human P-450 enzymes. (C) 2000 Elsevier Science Ltd.