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Journal ArticleDOI

Dissociation constants of fluorine-containing aliphatic amines

TLDR
In this paper, the dissociation constants of eight fluorine-containing propylamines were determined and the results obtained were correlated with the Taft substituent constant and compared with the literature data.
Abstract
1. The dissociation constants of eight fluorine-containing propylamines was determined. 2. The results obtained were correlated with the Taft substituent constant and compared with the literature data. 3. The constants ξ* from the equations derived for nonhalogen-containing amines are not applicable to the equations for the amines containing halogens.

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PatentDOI

Palladium-catalyzed arylation of fluoroalkylamines

TL;DR: The synthesis of fluorinated anilines by palladium-catalyzed coupling of fluoroalkylamines with aryl bromides and aryL chlorides is reported, and the fluoroalkylaniline products are unstable under typical conditions for C-N coupling reactions (heat and strong base).
Journal ArticleDOI

Loss of antagonistic activity of tamoxifen by replacement of one N-methyl of its side chain by fluorinated residues.

TL;DR: Efforts to limit the metabolic alteration of the aminoalkyl side chain of tamoxifen by fluorination largely decrease its ER-mediated antagonistic properties in MCF-7 cells.
Journal ArticleDOI

Potent Cytotoxic C-11 Modified Geldanamycin Analogues

TL;DR: Several 11-O-methyl-17-alkylaminogeldanamycin analogues were identified with improved potency relative to 17-AAG, and showed in vitro cytotoxicity against human cancer cell lines.
Journal ArticleDOI

Design of fluorinated 5-HT4R antagonists: Influence of the basicity and lipophilicity toward the 5-HT4R binding affinities

TL;DR: It is demonstrated that for this series, the affinity is decreased with decreased basicity of the piperidine's nitrogen atom, and the resulting increase in lipophilicity has minimal impact on binding affinity and selectivity.
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