quincorine,quinine,quincorine,quinine,sulfate,sulphate
INTRODUCTION
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Functionalized quinuclidines
are selective agonists and antagonists at a variety
of receptors (e.g. neurokinin-1 (NK1), 5-HT3, 5-HT4).
Particularly 3-substituted
quinuclidine derivatives have been identified as muscarinic
agonists with
potential for the treatment of Alzheimer's disease.
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Recently these quinuclidines are reported to be squalene synthase
inhibitors
which interrupts cholesterol biosynthesis. They also can be
used as an
anti-emetic in cancer chemotherapy (5-HT3
receptor antagonist) and
as muscarinic analgesic with potential treatment of
irritable bowel syndrome (IBS).
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CP
96, 345
NK1-receptor
antagonist
(Pfizer) |
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SB
202626
M1muscarinic
agonist
(SmithKline Beecham) |

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5-HT3-receptor
antagonist
(Syntex) |
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muscarinic
antagonist
(Pharmacia & Upjohn) |
ligand
for (R)-zacopride
binding site
(Roche Bioscience) |
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muscarinic
agonist
(Merck, Sharp & Dohme)
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squalen synthase inhibitor
(Zeneca)
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AF
102 B
muscarinic agonist
(Hoffmann-La Roche)
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..
Zeneca, Merck, Sharp and Dohme, SmithKline Beecham
Pharmaceuticals,
Syntex, Pfizer, Lilly, Astra AB and F. Hoffmann-La Roche LTD deal as
far as we know with the investigation of these quinuclidines
and the development of the adequate pharmaceuticals.
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See: |
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quincorine,
quinine,sulfate,QD, QCI,quincoridine,quincorine
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.Quinuclidines QCI & QCD |
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We are pleased to present our two new diastereomeric
enantiopure quinuclidines (1-azabicyclo[2.2.2]octanes):
Quincorine (QCI) (2S,4S,5R)-2-Hydroxymethyl-5-vinyl-quinuclidine and
Quincoridine (QCD) (2R,4S,5R)-2-Hydroxymethyl-5-vinyl-quinuclidine.
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Quincorine
(QCI) |
Quincoridine
(QCD) |
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The skeleton of Quincorine and Quincoridine
is identical to the framework
of the Cinchona alkaloids Quinine, Quinidine,
Cinchonidine and Cinchonine.
Extensive experience made during many decades can be used. |
The presented highly functionalized QCI
and QCD
possess 3 chiral centers and
are
valuable chiral building blocks for the pharmacology and medical
chemistry.
These
enantiopure compounds and their derivatives are also of
interest in combinatorial chemistry and in the development
of chiral ligands in asymmetric synthesis.
See:
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