ISSN:
0170-2041
Keywords:
Chemistry
;
Organic Chemistry
Source:
Wiley InterScience Backfile Collection 1832-2000
Topics:
Chemistry and Pharmacology
Description / Table of Contents:
Sila-Pharmaca, 361). - Sila-Procyclidine: A New Synthesis as well as Investigations of the Peripheral and Central Anticholinergic ActivityStarting with Cl3SiCH2Cl, sila-procyclidine (1b) as well as its derivatives 2b (sila-trihexyphenidyl), 3b, and 4b (sila-cycrimine) were prepared by a new six-step synthesis with a total yield of 16 (1b), 19 (2b), 8 (3b) and 7% (4b), respectively. - Comparative in vivo investigations (mice, per os administration) with respect to the peripheral and central anticholinergic activity have shown that the silicon compound 1b is advantageous over the carbon analogue 1a (procyclidine).
Notes:
Sila-Procyclidin (1b) sowie dessen Derivate 2b (Sila-Trihexyphenidyl), 3b und 4b (Sila-Cycrimin) wurden - ausgehend von Cl3SiCH2Cl - durch eine neue, sechsstufige Synthese mit einer Gesamtausbeute von 16 (1b), 19 (2b), 8 (3b) bzw. 7% (4b) dargestellt. - Vergleichende in-vivo-Untersuchungen (Maus, per-os-Applikation) hinsichtlich der peripheren und zentralen anticholinergen Wirkung haben gezeigt, daß die Silicium-Verbindung 1b dem Kohlenstoff-Analogon 1a (Procyclidin) überlegen ist.
Additional Material:
2 Ill.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1002/jlac.198719870109
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