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In contrast to the catalytic asymmetric dearomative reactions of indole substrates, those of the analogous benzofuran derivatives have been less explored. Here we report that the stereoselective domino Rauhut-Currier/Michael addition process of 3-benzofuranyl vinyl ketones and 3-olefinic (7-aza)oxindoles can be realised via catalysis by a chiral bifunctional phosphine, furnishing the previously unreported direct asymmetric dearomative reaction of benzofuran substrates tethered to a carbonyl group in a formal [4+2] cycloaddition manner. An array of hydrodibenzofuran derivatives with dense substitutions is generally constructed with excellent diastereoselectivity and enantioselectivity (up to >191 dr, >99% ee).

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H1219O – PubChem

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Provided herein are compounds, such as a compound of Formula (I), or a pharmaceutically acceptable salt thereof, that are immunoproteasome (such as LMP2 and LMP7) inhibitors. The compounds described herein can be useful for the treatment of diseases treatable by inhibition of immunoproteasomes. Also provided herein are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

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Benzofuran – Wikipedia,
Benzofuran | C8H1152O – PubChem

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Constructing fused hydrodibenzofuran architectures bearing a tetrasubstituted stereogenic center adjacent to an O atom is extremely difficult. Here we have developed an asymmetric dearomatizative Diels?Alder reaction using novel 2-(3-vinylbenzofuran-2-yl)ethan-1-one substrates and 3-olefinic 7-azaoxindoles. The reaction proceeds via in situ generation of a HOMO-raised formal trienamine species with a chiral primary amine catalyst, producing highly complex tetrahydrodibenzo[b,d]furan derivatives with vicinal tetrasubstituted stereogenic centers in moderate yields with excellent stereoselectivity (dr>19:1, up to 98% ee). (Figure presented.).

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H1218O – PubChem

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A series of symmetrically substituted 1,4-bis(3-aminopropyl)piperazines was synthesized and tested towards trypanothione reductase and for its in vitro trypanocidal potency. The most trypanocidal amongst them was found to be totally inactive towards the enzyme and thus constitutes a lead structure for the identification of new potential Trypanosoma cruzi target(s). (C) 2000 Elsevier Science Ltd.

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Benzofuran – Wikipedia,
Benzofuran | C8H1171O – PubChem

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Novel ABI-III compounds were designed and synthesized based on our previously reported ABI-I and ABI-II analogues. ABI-III compounds are highly potent against a panel of melanoma and prostate cancer cell lines, with the best compound having an average IC50 value of 3.8 nM. They are not substrate of Pgp and thus may effectively overcome Pgpmediated multidrug resistance. ABI-III analogues maintain their mechanisms of action by inhibition of tubulin polymerization.

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Benzofuran – Wikipedia,
Benzofuran | C8H1176O – PubChem

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A new method has been developed for the preparation of alpha,beta- unsaturated carboxylic acids and corresponding esters with (E)-stereoselectivity via the TiCl4-mediated olefination of aldehydes. The method, which uses readily available acetic acid or its alkyl esters as active methylene partners, is more flexible and complementary to conventional routes in the preparation of (E)-cinnamic acid derivatives.

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Benzofuran – Wikipedia,
Benzofuran | C8H1165O – PubChem

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Described herein are heteroaryl compounds with estrogen receptor modulation activity or function having the Formula (I), (II), and (III) structures: and stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I, II, and III compounds, as well as methods of using such estrogen receptor modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

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Benzofuran – Wikipedia,
Benzofuran | C8H1143O – PubChem

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Enantioenriched diaryl-, aryl heteroaryl-, and diheteroarylmethanols exhibit important biological and medicinal properties. One-pot catalytic asymmetric syntheses of these compounds beginning from readily available aryl bromides are introduced. Thus, lithium-bromide exchange with commercially available aryl bromides and n-BuLi was followed by salt metathesis with ZnCl2 to generate ArZnCl. A second equivalent of n-BuLi was added to form the mixed organozinc, ArZnBu. In the presence of enantioenriched amino alcohol-based catalysts, ArZnBu adds to aldehydes to afford essentially racemic diarylmethanols. The low enantioselectivities were attributed to a LiCl-promoted background reaction. To inhibit this background reaction, the chelating diamine TEEDA (tetraethylethylene diamine) was introduced prior to aldehyde addition. Under these conditions, enantioenriched diarylmethanols were obtained with >90% ee. Arylations of enals generated allylic alcohols with 81-90% ee. This procedure was unsuccessful, however, when applied to heteroaryl bromides, which was attributed to decomposition of the heteroaryl lithium under the salt metathesis conditions. To avoid this problem, the metathesis was conducted with EtZnCl, which enabled the salt metathesis to proceed at low temperatures. The resulting EtZn(ArHetero) intermediates (ArHetero ) 2-and 3-thiophenyl, 2-benzothiophenyl, 3-furyl, and 5-indolyl) were successfully added to aldehydes and heteroaryl aldehydes with enantioselectivities between 81-99%. These are the first examples of catalytic and highly enantioselective syntheses of diheteroarylmethanols. In a similar fashion, ferrocenyl bromide was used to generate FcZnEt and the ferrocenyl group added to benzaldehyde and heteroaromatic aldehydes to form ferrocene-based ligand precursors in 86-95% yield with 96-98% ee. It was also found that the arylation and heteroarylation of enals could be followed by diastereoselective epoxidations to provide epoxy alcohols with high enantio- and diastereoselectivities in a one-pot procedure.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H1206O – PubChem

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Disclosed are benzoheterocyclic alkylamine compounds, or a pharmaceutically acceptable salt thereof, or a stereoisomer thereof, and a preparation method thereof, and use of the same in the manufacture of an antibacterial drug as an inhibitor of staphyloxanthin synthesis in Staphylococcus aureus.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H1151O – PubChem

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Indolocarbazole glycosides are balanced between two conformations: a “closed” conformation containing a cyclic hydrogen bond between the indolocarbazole NH and the pyranose oxygen and an “open” conformation in which the indolocarbazole NH is hydrogen bonded to solvent. The open conformation never has a commanding advantage, even in DMSO, but in nonpolar environments the cyclic conformation predominates.

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Reference:
Benzofuran – Wikipedia,
Benzofuran | C8H1181O – PubChem