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Syntheses for the bis-O-trimethylsilylated (2), the tris-O,O,N-trimethylsilylated (3) and the tetrakis-O,O,N,N-trimethylsilylated dopamine (4) are described. The preparation of some N-trialkylsilylated 4,4-diphenylpiperidines 6-8 and of the N-triphenylsilylated piperidine 9 is also reported. The silylation of these neuropharmaca enhances their lipophilic character. Preliminary pharmacological investigations show the desired central effect of these compounds. The silylated dopamines 3 and 4 influence positively the rigid akinetic syndrom, which was induced by reserpine. The silylated 4,4-diphenylpiperidines 6-9 show the same effect on the content of neurotransmitters in the rat brain as the Antiparkinson drug 1-tert-butyl-4,4-diphenylpiperidine (budipine).

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Synthese und pharmakologische Eigenschaften von silylierten Dopaminen und 4.4-Diphenylpiperidinen/Synthesis and Pharmacological Properties of Silylated Dopamines and 4,4-Diphenylpiperidines