Azetidines

Moore, James A.; Ayers, Rita Seelig

doi:10.1002/9780470187197.ch1

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Cited by 24 publications

(1 citation statement)

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“…1 In contrast, the unsaturated and more strained 2-azetine (1,2-dihydroazete) system 1 (Figure 1) is comparatively less explored, which partly reflects issues of ease of access and stability (notably the propensity to undergo 4e electrocyclic ring-opening to 1-azabutadienes), although electron-withdrawing groups on the nitrogen are known to reduce instability. 2,3 …”

mentioning

confidence: 99%

Generation and Electrophile Trapping of N-Boc-2-lithio-2-azetine: Synthesis of 2-Substituted 2-Azetines

2014

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mentioning

confidence: 99%

Generation and Electrophile Trapping of N-Boc-2-lithio-2-azetine: Synthesis of 2-Substituted 2-Azetines

2014

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ChemInform Abstract: Azetidines

Moore¹,

Ayers²

1984

Chemischer Informationsdienst

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Preparation of a novel radiotracer targeting the EphB4 receptor via radiofluorination using spiro azetidinium salts as precursor

Wiemer

Steinbach

Pietzsch

et al. 2017

Labelled Comp Radiopharmac

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The visualization of Eph receptors, which are overexpressed in various tumor entities, using selective small molecule Eph inhibitors by means of positron emission tomography is a promising approach for tumor imaging. N-(Pyrimidinyl)indazolamines represent a class of compounds, which are known to have high affinity especially for the EphB4 receptor. Radiofluorination of these compounds could provide a highly specific imaging agent and was investigated using a classical nucleophilic introduction of [ F]fluoride as well as a less common nucleophilic ring-opening reaction of azetidinium salts. In the past, radiofluorinations using azetidinium precursors were demonstrated to result in high radiochemical yields in short periods. For this purpose, an azetidinium precursor based on the N-(pyrimidinyl)indazolamine lead compound was developed, and radiofluorination was successfully accomplished. The respective [ F]radiotracer was quickly prepared with high radiochemical purity >97% and in a radiochemical yield of 34%.

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Azetidines

Cited by 24 publications

References 369 publications

Generation and Electrophile Trapping of N-Boc-2-lithio-2-azetine: Synthesis of 2-Substituted 2-Azetines

Generation and Electrophile Trapping of N-Boc-2-lithio-2-azetine: Synthesis of 2-Substituted 2-Azetines

ChemInform Abstract: Azetidines

Preparation of a novel radiotracer targeting the EphB4 receptor via radiofluorination using spiro azetidinium salts as precursor

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