- Potential anxiolytic agents. 2. Improvement of oral efficacy for the pyrido[1,2-a]benzimidazole (PBI) class of GABA-A receptor modulators
-
We have further explored the structure-activity relationships of pyrido[1,2-α]benzimidazole (PBI) derivatives (viz. prototype 1), a novel series of central GABA-A receptor modulators, with the intent of enhancing oral efficacy. A study involving the introduction of acidic or basic groups led to the identification of RWJ-38293 (3a) as a potential anxiolytic agent.
- Maryanoff,McComsey,Ho,Shank,Dubinsky
-
-
Read Online
- Cu-Catalyzed Cross-Coupling of Nitroarenes with Aryl Boronic Acids to Construct Diarylamines
-
The development and study of a simple copper-catalyzed reaction of nitroarenes with aryl boronic acids to form diarylamines that uses phenyl silane as the stoichiometric terminal reductant is described. This cross-coupling reaction requires as little as 2 mol % of CuX and 4 mol % of diphosphine for success and tolerates a broad range of functional groups on either the nitroarene or the aryl boronic acid to afford the amine in good yield. Mechanistic investigations established that the cross-coupling reaction proceeds via a nitrosoarene intermediate and that copper is required to catalyze both the deoxygenation of the nitroarene to afford the nitrosoarene and C-NAr bond formation of the nitrosoarene with the aryl boronic acid.
- Guan, Xinyu,Zhu, Haoran,Driver, Tom G.
-
p. 12417 - 12422
(2021/10/12)
-
- SYNTHESIS OF META-SUBSTITUTED [18F]-3-FLUORO-4-AMINOPYRIDINES BY DIRECT RADIOFLUORINATION OF PYRIDINE N-OXIDES
-
Disclosed herein are methods for the fluorination aromatic N-heterocyclic N-oxides that comprise at least one leaving group. The N-oxides may be reduced to the fluorinated aromatic N-heterocyclic amine analogs. This novel fluorination approach may be successfully applied for synthesizing aromatic N-heterocyclic compounds labeled with 18F.
- -
-
Paragraph 0055
(2018/01/19)
-
- Synthesis of: Meta -substituted [18F]3-fluoro-4-aminopyridine via direct radiofluorination of pyridine N -oxides
-
Due to their electron-rich aromatic structure, nucleophilic (radio)fluorination of pyridines is challenging, especially at the meta position. In this paper, we describe the first example of direct fluorination of a pyridine N-oxide to produce a meta fluorinated pyridine. Specifically, fluorination of 3-bromo-4-nitropyridine N-oxide produced in several minutes 3-fluoro-4-nitropyridine N-oxide in moderate yield at room temperature. This intermediate compound was later converted to 3-fluoro-4-aminopyridine easily by catalytic hydrogenation. Furthermore, this approach was successfully applied for labeling with fluorine-18. The use of pyridine N-oxides for the preparation of fluoropyridines is unprecedented in the chemical literature and has the potential to offer a new way for the synthesis of these important structures in pharmaceuticals and radiopharmaceuticals.
- Brugarolas,Freifelder,Cheng,Dejesus
-
supporting information
p. 7150 - 7152
(2016/06/09)
-
- Peptide deformylase inhibitors
-
The present invention relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods directed to bacterial infections and inhibition of bacterial peptide deformylase (PDF) activity.
- -
-
Page/Page column
(2014/12/09)
-
- PEPTIDE DEFORMYLASE INHIBITORS
-
The present invention relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods directed to bacterial infections and inhi-bition of bacterial peptide deformylase (PDF) activity
- -
-
Page/Page column
(2014/02/15)
-
- Novel non-convalent thrombin inhibitors
-
The present invention provides compounds which have a pyrazinone or pyridinone ring at P3 and an optionally substituted heteroaryl group at P1. These compounds have biological activity as active and potent inhibitors of thrombin. Their pharmaceutically acceptable salts, pharmaceutical compositions thereof and methods of using these compounds and pharmaceutical compositions comprising these compounds as therapeutic agents for treatment of disease states in mammals which are characterized by abnormal thrombosis are also described.
- -
-
-
