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Mammary cancers are inhibited by administration of a combination of two drugs. The first compound is 6-hydroxy-2-(4-hydroxyphenyl)-3-[4-(2-pyrrolidinoethoxy)benzoyl]benzo[b]thiophene, and the second compound is tamoxifen.

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Benzothiophene – Wikipedia,
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The synthesis and advanced characterization of a series of extended dithieno[2,3-b:3′,2′-e][1,4-dihydro-1,4]phosphasilins is reported, and their suitability as new building blocks for organic electronics is evaluated. Synthesis of basic, as well as benzo-extended dithienophosphasilins, can be achieved using appropriate 2,3-dibromothiophene precursors in a two-step protocol introducing the silicon and phosphorus centers subsequently. Both ladder-type materials show the typical reactivity of trivalent phosphorus species and can quantitatively be converted into the corresponding oxides or gold complexes, the latter exemplified with the basic dithienophosphasilin. Their optoelectronic properties were found to be inferior to those of related dithieno[3,2-b:2′,3′-d]phospholes, indicating a disruption of the pi-conjugation in the molecular scaffold. X-ray crystallographic studies revealed that the molecular scaffold is planar in the oxidized benzo-extended material, whereas the basic dithieno materials show some small deviation from planarity. Density functional theory calculations suggest all materials to be planar, with the exception of the benzo-extended trivalent phosphasilin. This structure-property study illustrates that the disruption of the pi-conjugation in the molecular scaffold of the extended phosphasilins is exclusively due to the presence of the silicon center and its electronic effects, rather than structural features.

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A general procedure for the palladium-catalyzed carbonylative Sonogashira coupling of aryl bromides is reported, using near stoichiometric amounts of carbon monoxide. The method allows a broad substrate scope in moderate to excellent yields. The formed alkynone motive serves as a platform for synthesis of various heterocyclic structures, including pyrimidines. Furthermore, the presented strategy allows effective 13C labeling.

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A high yield synthesis of fluorescent benzo, thieno, and furo [c]-fused methyl 7-aryl-6H-pyrrolo[3,4-c]pyridazine-5-carboxylates, including unprecedented heterocyclic skeletons, was performed by the transformation of methyl 4-aminopyrrole-2-carboxylate into the corresponding diazo compound, followed by intramolecular azo coupling under acid conditions onto a nucleophilic aryl or hetaryl group in the 3-position. Azo coupling is completely regioselective and, according to DFT calculations, a kinetically controlled reaction. N-Methylation of 1,3-disubstituted 2H-pyrrolo[3,4-c]cinnolines occurs selectively at N5 under kinetic control, leading exclusively to 5-methyl-5H-pyrrolo[3,4-c]cinnoline derivatives.

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Compounds and compositions for modulating fibroblast activation protein (FAP) are described. The compounds and compositions may find use as therapeutic agents for the treatment of diseases, including hyperproliferative diseases.

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A zinc(II)/NHC system catalyzes the borylation of aryl halides with diboron (4) reagents in the presence of KOMe at rt. This transformation can be applied to a broad range of substrates with high functional group compatibility. Radical scavenger experiments do not support a radical-mediated process.

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A novel series of 2-benzothiophenealkylpiperazine derivatives 11 (a-d) with potential affinity at 5-HT1A serotonin receptors have been synthesized via solvent-free, microwave-promoted Michael addition of benzo[b]thiophene piperazine derivatives 6(a-c) to substituted benzo[b]thiophen-2-yl propenones 10(b,c).

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Friedel-Crafts acylation of arenes with methylthio- (1) or phenylthio-acetyl chloride (2) provides ready access to alpha-methylthio- or alpha-phenylthio-substituted acetophenones.The acyl chlorides 1 and 2 reacted also with organoaluminium reagents to give alpha-sulfenylated alkanones.

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Tricyclic oxindole carboxamides, prepared by (a) reaction of an isocyanate with the basic ring system or (b) ammonolysis of a corresponding alkyl ester, are non-steroidal antiinflammatory agents useful in the treatment of rheumatoid arthritis.

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We herein demonstrate that the combination of LiO-tBu, CsF, and [18]crown-6 efficiently promotes the direct C?H carboxylation of electron-rich heteroarenes (benzothiophene, thiophene, benzofuran, and furan derivatives). A variety of functional groups, including methyl, methoxy, halo, cyano, amide, and keto moieties, are compatible with this system. The reaction proceeds via the formation of a tert-butyl carbonate species.

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