551001-83-3

Upstream product

• 768-60-5 4-methoxyphenylacetylen 
• 1542908-88-2 6,8-dichloro-3-(4'-methoxyphenyl)coumarin 
• 60512-57-4 1-(2,2-dibromovinyl)-4-methoxybenzene 
• 120-83-2 2,4-dichlorophenol 
• 1321985-62-9 6-(β,β-dibromovinyl)-2,4-dichlorophenol 
• 13139-86-1 4-methoxyphenyl magnesium bromide 
• 1336808-79-7 5,7-dichloro-2-bromobenzo[b]furan 
• 1172576-91-8 diethyl(p-methoxyphenyl)aluminum 

Downstream Products

• 127988-86-7 4-(5,7-Dichloro-benzofuran-2-yl)-phenol 

Relevant academic research and scientific papers

Highly Efficient Synthesis of 2-Substituted Benzo[ b ]furan Derivatives from the Cross-Coupling Reactions of 2-Halobenzo[ b ]furans with Organoalane Reagents

A highly efficient and simple route for the synthesis of 2-substituted benzo[ b ]furans has been developed by palladium-catalyzed cross-coupling reaction of 2-halobenzo[ b ]furans with aryl, alkynyl, and alkylaluminum reagents. Various 2-aryl-, 2-alkynyl-, and 2-alkyl-substituted benzo[ b ]furan derivatives can be obtained in 23-97% isolated yields using 2-3 mol% PdCl 2/4-6 mol% XantPhos as the catalyst under mild reaction conditions. The aryls bearing electron-donating or electron-withdrawing groups in 2-halobenzo[ b ]furans gave products in 40-97% isolated yields. In addition, aluminum reagents containing thienyl, furanyl, trimethylsilanyl, and benzyl groups worked efficiently with 2-halobenzo[ b ]furans as well, and three bioactive molecules with 2-substituted benzo[ b ]furan skeleton were synthesized. Furthermore, the broad substrates scope and the typical maintenance of vigorous efficiency on gram scale make this protocol a potentially practical method to synthesize 2-substituted benzo[ b ]furan derivatives. On the basis of the experimental results, a possible catalytic cycle has been proposed.

Preparation method of benzofuran derivative

The invention belongs to the field of organic chemical synthesis, and particularly relates to a preparation method of a benzofuran derivative. According to the specific technical scheme, the preparation method of the benzofuran derivative comprises the fo

2-Phenylbenzo[b]furans: Synthesis and promoting activity on estrogen biosynthesis

Estrogen biosynthesis is pivotal to many physiological processes of human. Aberrant estrogen level is closely related to a variety of diseases, including breast cancer and osteoporosis. Previously we found that 2-phenylbenzo[b]furan glycosides could promote estrogen biosynthesis. To find high active 2-phenylbenzo[b]furans, fifty-four 2-phenylbenzo[b]furans were prepared via four strategies according to corresponding substrate scopes. Biological evaluation in HEK293A cells showed that some compounds exhibited promotive activity on estrogen biosynthesis. 2-(4-Chlorophenyl)-7-methoxybenzo[b]furan possessed the highest activity with EC50value of 14.68?μM. Furthermore, these compounds did not affect aromatase expression in HEK292A cells, indicating that these 2-phenylbenzo[b]furans might enhance estrogen biosynthesis via directly allosteric regulation of aromatase or indirectly via posttranslational modification.

A concise route to functionalized benzofurans directly from gem-dibromoalkenes and phenols

A tandem strategy for the construction of benzofuran motifs has been developed directly from gem-dibromoalkenes and phenols under palladium-catalyzed conditions. This flexible and novel methodology provides direct access to 2-aryl and 2-styryl benzofurans

Copper-catalyzed decarboxylative intramolecular C-O coupling: Synthesis of 2-arylbenzofuran from 3-arylcoumarin

A copper-catalyzed decarboxylative intramolecular C-O coupling reaction was established. Under aerobic conditions in the presence of cupric chloride/1,10-phenathroline, a variety of 2-arylbenzofurans were prepared from 3-arylcoumarins in one-pot with yields from 26% to 84%. The Royal Society of Chemistry 2014.

PHARMACEUTICAL COMPOSITIONS AND METHODS OF PREVENTING, TREATING, OR INHIBITING INFLAMMATORY DISEASES, DISORDERS, OR CONDITIONS OF THE SKIN, AND DISEASES, DISORDERS, OR CONDITIONS ASSOCIATED WITH COLLAGEN DEPLETION

The present invention provides compositions and methods for preventing, treating, or inhibiting inflammatory diseases, disorders, or conditions of the skin, and diseases, disorders, or conditions associated with collagen depletion using one or more estrogenic agents.

Substituted 2-phenyl benzofurans as estrogenic agents

This invention provides estrogen receptor modulators of formula I, having the structure wherein R, R′, A, A′, X, Y, and Y are as defined in the specification, or a pharmaceutically acceptable salt thereof.