- Synthesis of beta-proline like derivatives and their evaluation as sodium channel blockers
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(Chemical Equation Presented) A simple and convenient procedure for the preparation of beta-proline like derivatives in their racemic and optically active forms has been reported. The compounds have been screened for their potential activity as sodium cha
- Muraglia, Marilena,Franchini, Carlo,Corbo, Filomena,Scilimati, Antonio,Sinicropi, Maria Stefania,De Luca, Annamaria,De Bellis, Michela,Camerino, Diana Conte,Tortorella, Vincenzo
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p. 1099 - 1103
(2008/09/17)
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- 1-SUBSTITUTED-3-PYRROLIDINE DERIVATIVES AS MUSCARINIC RECEPTOR ANTAGONISTS
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This invention generally relates to the derivatives of 1 -substituted-3 -pyrroli dines having the structure of Formula (I): The compounds of this invention can function as..muscarinic receptor antagonists, and can be used for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to a process for the preparation of the compounds of the present invention. pharmaceutical compositions containing the compounds of the present invention and the methods for treating the diseases mediated through muscarinic receptors.
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- Novel farnesyl protein transferase inhibitors as antitumor agents
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Disclosed are novel tricyclic compounds represented by the formula (1.0): or a pharmaceutically acceptable salt or solvate thereof. The compounds are useful for inhibiting farnesyl protein transferase. Also disclosed are pharmaceutical compositions comprising compounds of formula 1.0. Also disclosed are methods of treating cancer using the compounds of formula 1.0.
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- Process for preparing 2-phenyl-3-naphthylpropionic acid derivatives
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A process for preparing a compound represented by general formulae (5) and (6) in the following reaction scheme or salts thereof, wherein R1represents a protective group for a nitrogen atom; R2represents a methanesulfonyl group or p-
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- Efficient synthesis of the 5-HT2C receptor agonist, Org 37684
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An efficient synthesis of the 5-HT2C receptor agonist Org 37684 is presented. The synthesis utilises the regioselective demethylation of an arylether as the key step.
- Adams,Duncton
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p. 2029 - 2036
(2007/10/03)
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- Synthesis and structure-activity relationships of naphthamides as dopamine D3 receptor ligands
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A series of naphthamides were synthesized, and the affinities of these compounds were determined for dopamine D2 and D3 receptors using radioligand binding techniques. The naphthamide compounds that were prepared include N-(1- alkylp
- Huang,Luedtke,Freeman,Wu,Mach
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p. 1815 - 1826
(2007/10/03)
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- Derivatives of azetidine and pyrrolidine
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The invention relates to a compound having formula (I) wherein A is an optionally unsaturated 5- or 6-membered ring, which may comprise a heteroatom selected from N, O and S and which may be substituted with oxo or (1-6C)alkyl; R1, R2and R3are independently H, (1-6C)alkyl, (1-6C)alkoxy, (1-6C)alkoxy(1-6C)-alkyl, carbo(1-6C)alkoxy or halogen; X is O or S; and n is 1 or 2; or a pharmaceutically acceptable salt thereof, with the exception of 3-(naphth-1-yl-oxy)-pyrolidin and 3-(5,6,7,8-tetmhydro-naphth-1-yl-oxy)-pyrolidin. The compounds of the invention have antidepressant activity and can be used in treating or preventing serotonin-related diseases.
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- A practical ex-chiral-pool synthesis of β-proline and homo-β-proline
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Starting from aspartic acid an efficient synthesis of enantiomerically pure β-proline and homo-β-proline is described. The key step of the synthesis includes formation of the 1,4-biselectrophile 6, followed by rearrangement via the aziridinium intermediate 7 and ring closure to give the pyrrolidinium salt 9a which can serve as a common precursor for both target compounds.
- Thomas, Christoph,Orecher, Florian,Gmeiner, Peter
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p. 1491 - 1496
(2007/10/03)
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- Derivatives of azetidine and pyrrolidine
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The invention relates to a compound having the formula I wherein A is an optionally unsaturated 5- or 6-membered ring, which may comprise a heteroatom selected from N, O and S and which may be substituted with oxo or (1-6C)alkyl; R1, R2and R3are independently H, (1-6C)alkyl, (1-6C)alkoxy, (1-6C)alkoxy-(1-6C)alkyl, carbo(1-6C)alkoxy or halogen; X is O or S; and n is 1 or 2; or a pharmaceutically acceptable salt thereof, with the exception of 3-(naphth-1-yl-oxy)-pyrrolidin and 3-(5,6,7,8-tetrahydro-naphth-1-yl-oxy)-pyrrolidin., The compounds of the invention have antidepressant activity and can be used in treating or preventing serotonin-related diseases.
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- 2-Dibenzylaminobutane-1,4-diol: A Versatile Intermediate for a Chirospecific β-amino Acid Synthesis
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Starting from the chiral building block 1, which is readily available from natural aspartic acid, a concise and versatile synthesis of optically active β-amino acids including β-proline derivatives is reported.Regioselective transformations of the 1,4-bis-electrophile 2 are facilitated by an anchimeric participation.
- Gmeiner, Peter,Orecher, Florian,Thomas, Christoph,Weber, Klaus
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p. 381 - 382
(2007/10/02)
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- An Efficient Method for the Synthesis of (R)-3-(1-Amino-1-methylethyl)pyrrolidines for the Antiinfective Agent, PD 138312
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Methylcerium dichloride has been found to undergo bis addition to nitriles to produce tertiary carbinamines with retention of optical purity at the ? position.This result is used in the development of a short, economical synthesis of the 1,8-naphthyridine antiinfective agent, PD 138312.
- Fedij, Victor,Lenoir, Edward A.,Suto, Mark J.,Zeller, James R.,Wemple, James
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p. 1131 - 1134
(2007/10/02)
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- Process for chiral 3-(1-amino-1,1-bisalkylmethyl)-1-substituted-pyrrolidines
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The process for the preparation of chiral 3-(1-amino-1,1-bisalkylmethyl)-1-substituted-pyrrolidines used as key intermediates for the preparation of naphthyridine and quinolone antibacterial agents which comprises reacting readily available chiral 1-subst
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- Asymmetric Synthesis and Properties of the Enantiomers of the Antibacterial Agent 7-(3-Aminopyrrolidin-1-yl)-1-(2,4-difluorophenyl)-1,4-dihydro-6-fluoro-4-oxo-1,8-naphthyridine-3-carboxylic Acid Hydrochloride
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Compound 1 is a potent member of the quinoloecarboxylic acid class of antibacterial agents and is currently undergoing clinical evaluation.We have developed efficient asymmetric syntheses of the enantiomers of this agent.The S-(+) enantiomer 1a is 1-2 log2 dilutions more active than the R-(-) enantiomer 1b against aerobic bacteria and 1-2 or more log2 dilutions more active against anaerobic bacteria in vitro.The enantiomer 1a shows significantly better in vivo activity in a Pseudomonas aeruginosa mouse protection model compared to racemic 1.Coupled with the improved solubility profile of 1a relative to racemic material, these features may be of practical significance from a clinical standpoint.
- Rosen, Terry,Chu, Daniel T. W.,Lico, Isabella M.,Fernandes, Prabhavathi B.,Shen, Linus,et al.
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p. 1586 - 1590
(2007/10/02)
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