Pharmacokinetics of panomifene in healthy volunteers at phase I/a study

Erdélyi-Tóth, V.; Gyergyay, Fruzsina; Számel, I.; Pap, Erna; Kralovánszky, Judit; Bojti, Erzsébet; Csörgö, M.; Drabant, Sándor; Klebovich, Imre

doi:10.1097/00001813-199707000-00008

Cited by 17 publications

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“…Incorporation of the trifluoromethyl group (CF 3 ) into alkenes can enhance their properties and modulate reactivities. Notably, many pharmaceuticals [4–7] and agrochemicals [8] feature vinyl‐CF 3 moieties (Figure 1), which impart unique physicochemical characteristics in drug metabolism and pharmacopathology. For example, Fludelone, [4] derived from Epothilone D [7] by replacement of the methyl group with a trifluoromethyl one, exhibits superior metabolism stability while maintaining the antitumor efficacy.…”

Section: Introductionmentioning

confidence: 99%

Hydroxylamine‐Mediated C(sp²)−H Trifluoromethylation of Terminal Alkenes

Zhao,

Zhong,

Dong

et al. 2024

Chemistry A European J

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Introduction of the trifluoromethyl (CF3) group into organic compounds has garnered substantial interest because of its significant role in pharmaceuticals and agrochemicals. Here, we report a hydroxylamine‐mediated radical process for C(sp2)−H trifluoromethylation of terminal alkenes. The reaction shows good reactivity, impressive E/Z selectivity (up to > 20:1), and broad functional group compatibility. Expansion of this approach to perfluoroalkylation and late‐stage trifluoromethylation of bioactive molecules demonstrates its promising application potential. Mechanistic studies suggest that the reaction follows a radical addition and subsequent elimination pathway.

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Section: Introductionmentioning

confidence: 99%

Hydroxylamine‐Mediated C(sp²)−H Trifluoromethylation of Terminal Alkenes

Zhao,

Zhong,

Dong

et al. 2024

Chemistry A European J

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“…Incorporation of fluorine into molecules can bring notable changes in physical and chemical properties . Among them, trifluoromethyl group is one of the most important fluorine-containing functional groups for its addition of metabolic stability and lipophilicity .…”

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confidence: 99%

Enantioselective N-Heterocyclic Carbene-Catalyzed Synthesis of Trifluoromethyldihydropyridinones

et al. 2015

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Recent Advances in the Synthesis of Tamoxifen and Analogues in Medicinal Chemistry

et al. 2020

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Tamoxifen is one of the important tricyclicethylene moieties and recognized as an important drug candidate because of extensive applications in the field of medicinal and pharmaceutical chemistry. Recently, ample attention is given to this analogue by organic and medicinal chemistry community due to its successful utilization for the inhibition of estrogen receptor in MCF-7 breast cancer cell lines. Due to its structural character, tamoxifen is also useful in material chemistry. The synthesis of tamoxifen and its anlogues is desirable from easily available chemicals as an important drug candidate. Here, we report a review on various synthetic schemes for tamoxifen and its anlogues employing use of different strategies such as formation of CÀ C, C=C and C�C bonds, CÀ H functionalization, addition to alkynes, insertion reaction, nucleophilic substitution and addition reactions, elimination reaction, reductive couplings etc.

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Pharmacokinetics of panomifene in healthy volunteers at phase I/a study

Cited by 17 publications

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Hydroxylamine‐Mediated C(sp²)−H Trifluoromethylation of Terminal Alkenes

Hydroxylamine‐Mediated C(sp²)−H Trifluoromethylation of Terminal Alkenes

Enantioselective N-Heterocyclic Carbene-Catalyzed Synthesis of Trifluoromethyldihydropyridinones

Recent Advances in the Synthesis of Tamoxifen and Analogues in Medicinal Chemistry

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Pharmacokinetics of panomifene in healthy volunteers at phase I/a study

Cited by 17 publications

References 0 publications

Hydroxylamine‐Mediated C(sp2)−H Trifluoromethylation of Terminal Alkenes

Hydroxylamine‐Mediated C(sp2)−H Trifluoromethylation of Terminal Alkenes

Enantioselective N-Heterocyclic Carbene-Catalyzed Synthesis of Trifluoromethyldihydropyridinones

Recent Advances in the Synthesis of Tamoxifen and Analogues in Medicinal Chemistry

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Hydroxylamine‐Mediated C(sp²)−H Trifluoromethylation of Terminal Alkenes

Hydroxylamine‐Mediated C(sp²)−H Trifluoromethylation of Terminal Alkenes