63260-82-2Relevant academic research and scientific papers
MUSCARINIC MODULATORS
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Page/Page column 56-57, (2010/11/24)
The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.
The conversion of amides to esters with Meerwein's reagent. Application to the synthesis of a carfentanil precursor
Kiessling, Anthony J.,McClure, Cynthia K.
, p. 923 - 937 (2007/10/03)
An efficient two step transformation of 1°and 2°amides to methyl and ethyl esters has been developed using trimethyl- and triethyloxonium tetrafluoroborates, and dilute acid. This methodology was applied to 1-benzyl-4-phenylamino-4-piperidinecarboxamide, a precursor in the synthesis of carfentanil, to produce the methyl ester in 60% yield and the ethyl ester in 80% yield.
Synthesis and pharmacological evaluation of 4,4-disubstituted piperidines
Colapret,Diamantidis,Spencer,Spaulding,Rudo
, p. 968 - 974 (2007/10/02)
A new class of piperidine derivatives is added to the increasing family of compounds related to fentanyl and carfentanil. Herein, we describe the synthesis and pharmacology of a number of 1-(arylethyl)-4-(acylamino)-4-[(acyloxy)-methyl]piperidines such as 9, 15, and 23. As expected, many of these congeners of fentanyl are extremely potent narcotic agonists. The aim of the study was to identify short-acting analgesic agents (i.e. less than 6 min in the mouse hot-plate assay) for possible use in the surgical theater. Many of the drugs proved to be of intermediate and long duration (i.e. 6-15 min and > 15 min, respectively). In addition to analgesic activity, many of the compounds exhibited anesthetic properties as well. The structure-activity relationship for these entities is presented and discussed.
THE SYNTHESIS OF 1,8-DIAZASPIRO-DECANES
Parys, Marc Van,Vandewalle, Maurits
, p. 749 - 756 (2007/10/02)
The synthesis of some substituted 1,8-diazaspirodecanes starting from 1-benzyl-4-oxo-piperidine is described.This skeleton is isosteric to the 1,3,8-triazaspiro-decane structure present in important neuroleptic agents.
N-Aryl-N-(1-L-4-piperidinyl)-arylacetamides
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, (2008/06/13)
Novel N-aryl-N-(1-L-4-piperidinyl)arylacetamides useful as anti-arrhythmic agents, a method of treating arrhythmia which comprises the systemic administration of such compounds to warm-blooded animals and pharmaceutical compositions to be used therefor.
N-aryl-N-(1-alkyl-4-piperidinyl)-arylacetamides
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, (2008/06/13)
Novel N-aryl-N-(1-L-4-piperidinyl)arylacetamides useful as antiarrhythmic agents, a method of treating arrhythmia which comprises the systemic administration of such compounds to warm-blooded animals and pharmaceutical compositions to be used therefor.
