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Aliphatic Substitution

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J L Duff – One of the best experts on this subject based on the ideXlab platform.

  • single electron transfer in nucleophilic Aliphatic Substitution evidence for single electron transfer in the reactions of 1 halonorbornanes with various nucleophiles
    Journal of Organic Chemistry, 1994
    Co-Authors: E C Ashby, J L Duff

    Abstract:

    A series of 1-halonorbornanes was used as a model system in reactions with severqal nucleophiles in order to determine the involvement of single electron transfer (SET) in nucleophilic Aliphatic Substitution in the absence of light. The 1-halonorbornanes were allowed to react with Me 3 Sn – , Ph 2 P – , AlH 4 – , N(iPr) 2 – , SPh – , and the 2-nitropropyl anion in ether solvents at room temperature to 0 o C. The results of product anlyses, the use of radical and radical anion trapping reagents, the results of deuterium labeling studies, and the nucleofugality effect support a SET mechanism for the reactions involving 1-iodonorbomane

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Nunzio Denora – One of the best experts on this subject based on the ideXlab platform.

  • A Novel PET Imaging Probe for the Detection and Monitoring of Translocator Protein 18 kDa Expression in Pathological Disorders
    Scientific Reports, 2016
    Co-Authors: Mara Perrone, Byung Seok Moon, Hyun Soo Park, Valentino Laquintana, Jae Ho Jung, Annalisa Cutrignelli, Angela Lopedota, Massimo Franco, Nunzio Denora

    Abstract:

    A new fluorine-substituted ligand, compound 1 (CB251), with a very high affinity (Ki = 0.27 ± 0.09 nM) and selectivity for the 18-kDa translocator protein (TSPO), is presented as an attractive biomarker for the diagnosis of neuroinflammation, neurodegeneration and tumour progression. To test compound 1 as a TSPO PET imaging agent in vivo , 2-(2-(4-(2-[^18F]fluoroethoxy)phenyl)-6,8-dichloroimidazo[1,2-a]pyridin-3-yl)- N,N -dipropylacetamide ([^18F] 1 ; [^18F]CB251) was synthesized by nucleophilic Aliphatic Substitution in a single-step radiolabelling procedure with a 11.1 ± 3.5% ( n  = 14, decay corrected) radiochemical yield and over 99% radiochemical purity. In animal PET imaging studies, [^18F]CB251 provided a clearly visible image of the inflammatory lesion with the binding potential of the specifically bound radioligand relative to the non-displaceable radioligand in tissue (BP_ND 1.83 ± 0.18), in a neuroinflammation rat model based on the unilateral stereotaxic injection of lipopolysaccharide (LPS), comparable to that of [^11C]PBR28 (BP_ND 1.55 ± 0.41). [^18F]CB251 showed moderate tumour uptake (1.96 ± 0.11%ID/g at 1 h post injection) in human glioblastoma U87-MG xenografts. These results suggest that [^18F]CB251 is a promising TSPO PET imaging agent for neuroinflammation and TSPO-rich cancers.

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Mara Perrone – One of the best experts on this subject based on the ideXlab platform.

  • A Novel PET Imaging Probe for the Detection and Monitoring of Translocator Protein 18 kDa Expression in Pathological Disorders
    Scientific Reports, 2016
    Co-Authors: Mara Perrone, Byung Seok Moon, Hyun Soo Park, Valentino Laquintana, Jae Ho Jung, Annalisa Cutrignelli, Angela Lopedota, Massimo Franco, Nunzio Denora

    Abstract:

    A new fluorine-substituted ligand, compound 1 (CB251), with a very high affinity (Ki = 0.27 ± 0.09 nM) and selectivity for the 18-kDa translocator protein (TSPO), is presented as an attractive biomarker for the diagnosis of neuroinflammation, neurodegeneration and tumour progression. To test compound 1 as a TSPO PET imaging agent in vivo , 2-(2-(4-(2-[^18F]fluoroethoxy)phenyl)-6,8-dichloroimidazo[1,2-a]pyridin-3-yl)- N,N -dipropylacetamide ([^18F] 1 ; [^18F]CB251) was synthesized by nucleophilic Aliphatic Substitution in a single-step radiolabelling procedure with a 11.1 ± 3.5% ( n  = 14, decay corrected) radiochemical yield and over 99% radiochemical purity. In animal PET imaging studies, [^18F]CB251 provided a clearly visible image of the inflammatory lesion with the binding potential of the specifically bound radioligand relative to the non-displaceable radioligand in tissue (BP_ND 1.83 ± 0.18), in a neuroinflammation rat model based on the unilateral stereotaxic injection of lipopolysaccharide (LPS), comparable to that of [^11C]PBR28 (BP_ND 1.55 ± 0.41). [^18F]CB251 showed moderate tumour uptake (1.96 ± 0.11%ID/g at 1 h post injection) in human glioblastoma U87-MG xenografts. These results suggest that [^18F]CB251 is a promising TSPO PET imaging agent for neuroinflammation and TSPO-rich cancers.

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  • A Novel PET Imaging Probe for the Detection and Monitoring of Translocator Protein 18 kDa Expression in Pathological Disorders
    Scientific Reports, 2016
    Co-Authors: Mara Perrone, Byung Seok Moon, Hyun Soo Park, Valentino Laquintana, Jae Ho Jung, Annalisa Cutrignelli, Angela Lopedota, Massimo Franco

    Abstract:

    A new fluorine-substituted ligand, compound 1 (CB251), with a very high affinity (Ki = 0.27 ± 0.09 nM) and selectivity for the 18-kDa translocator protein (TSPO), is presented as an attractive biomarker for the diagnosis of neuroinflammation, neurodegeneration and tumour progression. To test compound 1 as a TSPO PET imaging agent in vivo, 2-(2-(4-(2-[18F]fluoroethoxy)phenyl)-6,8-dichloroimidazo[1,2-a]pyridin-3-yl)-N,N-dipropylacetamide ([18F]1; [18F]CB251) was synthesized by nucleophilic Aliphatic Substitution in a single-step radiolabelling procedure with a 11.1 ± 3.5% (n = 14, decay corrected) radiochemical yield and over 99% radiochemical purity. In animal PET imaging studies, [18F]CB251 provided a clearly visible image of the inflammatory lesion with the binding potential of the specifically bound radioligand relative to the non-displaceable radioligand in tissue (BPND 1.83 ± 0.18), in a neuroinflammation rat model based on the unilateral stereotaxic injection of lipopolysaccharide (LPS), comparable to that of [11C]PBR28 (BPND 1.55 ± 0.41). [18F]CB251 showed moderate tumour uptake (1.96 ± 0.11%ID/g at 1 h post injection) in human glioblastoma U87-MG xenografts. These results suggest that [18F]CB251 is a promising TSPO PET imaging agent for neuroinflammation and TSPO-rich cancers.

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