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Buchler GmbH
D-38110 Braunschweig
Ütteler Strasse 3
Tel.  ++ 49  5307  93121

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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.


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).

CP 96, 345
NK1-receptor antagonist

SB 202626
muscarinic  agonist
(SmithKline Beecham)

5-HT3-receptor antagonist

muscarinic antagonist
(Pharmacia & Upjohn)

ligand for (R)-zacopride
binding site
(Roche Bioscience)

muscarinic agonist
(Merck, Sharp & Dohme)

squalen synthase inhibitor

AF 102 B
muscarinic agonist
(Hoffmann-La Roche)

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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quincorine, quinine,sulfate,QD, QCI,quincoridine,quincorine

.Quinuclidines QCI & QCD

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

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Quincorine (QCI)

Quincoridine (QCD)


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.


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