945978-64-3Relevant articles and documents
Access to Aryl and Heteroaryl Trifluoromethyl Ketones from Aryl Bromides and Fluorosulfates with Stoichiometric CO
Johansen, Martin B.,Gedde, Oliver R.,Mayer, Thea S.,Skrydstrup, Troels
, p. 4068 - 4072 (2020/06/03)
We report a sequential one-pot preparation of aromatic trifluoromethyl ketones starting from readily accessible aryl bromides and fluorosulfates, the latter easily prepared from the corresponding phenols. The methodology utilizes low pressure carbon monoxide generated ex situ from COgen to generate Weinreb amides as reactive intermediates that undergo monotrifluoromethylation affording the corresponding aromatic trifluoromethyl ketones (TFMKs) in good yields. The stoichiometric use of CO enables the possibility for accessing 13C-isotopically labeled TFMK by switching to the use of 13COgen.
METHODS OF USING AND COMPOSITIONS COMPRISING TRYPTOPHAN HYDROXYLASE INHIBITORS
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, (2009/01/24)
Methods and compositions comprising tryptophan hydroxylase inhibitors are disclosed. Particular methods are directed at reducing or avoiding serotonin-mediated adverse effects associated with some drugs.
Modulation of peripheral serotonin levels by novel tryptophan hydroxylase inhibitors for the potential treatment of functional gastrointestinal disorders
Shi, Zhi-Cai,Devasagayaraj, Arokiasamy,Gu, Kunjian,Jin, Haihong,Marinelli, Brett,Samala, Lakshman,Scott, Sheldon,Stouch, Terry,Tunoori, Ashok,Wang, Ying,Zang, Yi,Zhang, Chengmin,Kimball, S. David,Main, Alan J.,Sun, Weimei,Yang, Qi,Nouraldeen, Amr,Yu, Xiang-Qing,Buxton, Eric,Patel, Shiv,Nguyen, Nghi,Swaffield, Jon,Powell, David R.,Wilson, Alan,Liu, Qingyun
supporting information; experimental part, p. 3684 - 3687 (2009/04/06)
The discovery of a novel class of peripheral tryptophan hydroxylase (TPH) inhibitors is described. This class of TPH inhibitors exhibits excellent potency in in vitro biochemical and cell-based assays, and it selectively reduces serotonin levels in the murine intestine after oral administration without affecting levels in the brain. These TPH1 inhibitors may provide novel treatments for gastrointestinal disorders associated with dysregulation of the serotonergic system, such as chemotherapy-induced emesis and irritable bowel syndrome.