4 research outputs found
<sup>18</sup>F‑Deoxyfluorination of Phenols via Ru π‑Complexes
No full textThe deficiency of robust and practical
methods for <sup>18</sup>F-radiofluorination is a bottleneck for positron
emission tomography
(PET) tracer development. Here, we report the first transition-metal-assisted <sup>18</sup>F-deoxyfluorination of phenols. The transformation benefits
from readily available phenols as starting materials, tolerance of
moisture and ambient atmosphere, large substrate scope, and translatability
to generate doses appropriate for PET imaging
<sup>18</sup>F‑Deoxyfluorination of Phenols via Ru π‑Complexes
No full textThe deficiency of robust and practical
methods for <sup>18</sup>F-radiofluorination is a bottleneck for positron
emission tomography
(PET) tracer development. Here, we report the first transition-metal-assisted <sup>18</sup>F-deoxyfluorination of phenols. The transformation benefits
from readily available phenols as starting materials, tolerance of
moisture and ambient atmosphere, large substrate scope, and translatability
to generate doses appropriate for PET imaging
<sup>18</sup>F‑Deoxyfluorination of Phenols via Ru π‑Complexes
No full textThe deficiency of robust and practical
methods for <sup>18</sup>F-radiofluorination is a bottleneck for positron
emission tomography
(PET) tracer development. Here, we report the first transition-metal-assisted <sup>18</sup>F-deoxyfluorination of phenols. The transformation benefits
from readily available phenols as starting materials, tolerance of
moisture and ambient atmosphere, large substrate scope, and translatability
to generate doses appropriate for PET imaging
Development of a Fluorinated Class‑I HDAC Radiotracer Reveals Key Chemical Determinants of Brain Penetrance
No full textDespite
major efforts, our knowledge about many brain diseases
remains remarkably limited. Epigenetic dysregulation has been one
of the few leads toward identifying the causes and potential treatments
of psychiatric disease over the past decade. A new positron emission
tomography radiotracer, [<sup>11</sup>C]ÂMartinostat, has enabled the
study of histone deacetylase in living human subjects. A unique property
of [<sup>11</sup>C]ÂMartinostat is its profound brain penetrance, a
feature that is challenging to engineer intentionally. In order to
understand determining factors for the high brain-uptake of Martinostat,
a series of compounds was evaluated in rodents and nonhuman primates.
The study revealed the major structural contributors to brain uptake,
as well as a more clinically relevant fluorinated HDAC radiotracer
with comparable behavior to Martinostat, yet longer half-life
