- MUSCARINIC MODULATORS
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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.
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Page/Page column 56-57
(2010/11/24)
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- The conversion of amides to esters with Meerwein's reagent. Application to the synthesis of a carfentanil precursor
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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.
- Kiessling, Anthony J.,McClure, Cynthia K.
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p. 923 - 937
(2007/10/03)
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- Synthesis and pharmacological evaluation of 4,4-disubstituted piperidines
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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.
- Colapret,Diamantidis,Spencer,Spaulding,Rudo
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p. 968 - 974
(2007/10/02)
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- THE SYNTHESIS OF 1,8-DIAZASPIRO-DECANES
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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.
- Parys, Marc Van,Vandewalle, Maurits
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p. 749 - 756
(2007/10/02)
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- N-Aryl-N-(1-L-4-piperidinyl)-arylacetamides
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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.
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- N-aryl-N-(1-alkyl-4-piperidinyl)-arylacetamides
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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.
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