120115-93-7Relevant academic research and scientific papers
RECEPTOR REGULATOR
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, (2010/02/13)
A compound having a partial structure represented by the formula (A) (wherein ring Xa represents a nitrogen-containing ring and R represents optionally substituted amino) or a salt thereof. The compound or salt is highly effective in regulating neuromedin U receptors and is useful as a preventive/therapeutic agent for hypertension, etc.
4-phenyl- and 4-heteroaryl-4-anilidopiperidines. A novel class of analgesic and anesthetic agents
Kudzma,Severnak,Benvenga,Ezell,Ossipov,Knight,Rudo,Spencer,Spaulding
, p. 2534 - 2542 (2007/10/02)
The incorporation of the 4-phenylpiperidine pharmacophore found in morphine into 4-anilidopiperidines related to fentanyl led to a novel class of potent opioid analgesic and anesthetic agents with a favorable pharmacological profile. The synthesis analgesic activity, and anesthetic properties of a series of 4-phenyl-4-anilidopiperidines (13-29) are discussed. Isosteric replacement of the phenyl by various heteroaryl substituents extended the series to include 4-heteroaryl-4-anilidopiperidines (30-53). Within this group, 1-[2-(1H-pyrazol-1-yl)ethyl]4-4(4-methylthiazol-2-yl)-4-(N- phenylpropionamido)piperidine (48), exhibited high analgesic potency, short duration of action, rapid recovery of motor coordination following anesthetic doses, and greater cardiovascular and respiratory safety during anesthesia as compared with opioids fentanyl (1) and alfentanil (2) currently in clinical use. Such analgesics could be of great utility to clinicians in the expanding outpatient surgical arena and for patient-controlled analgesia and computer assisted continuous infusion pain control techniques.
A VARIANT OF THE BRUYLANTS REACTION. SYNTHESIS OF 4-HETEROARYL-4-ANILINOPIPERIDINES.
Kudzma, Linas V.,Spencer, H. Kenneth,Severnak, Sherry A.
, p. 6827 - 6830 (2007/10/02)
Imines can be generated in situ from α-aminonitriles and efficiently trapped by a variety of lithiated heterocycles.This variation of the Bruylants reaction has proven to be a general method for the synthesis of α-heteroaryl secondary amines.
