Biomedical subjects
Publications and source records attributed to K Posselt.
Starting from hellebrigenin, orally cardiotonic active acylcardiosteroid derivatives have been synthesized. D 12316 (acrihellin), the hellebrigenin-3 beta-dimethylacrylate, has been chosen for clinical evaluation.
A review on new cerebrally active basic dithienyl compounds related to (+)-(R)-alpha-((S)-1-[(3,3-di-3-thienylallyl)amino]-ethyl)-benzylalcohol (tinofedrine) is presented. Tinofedrine was selected out of a large number of related compounds on account of its high increase of cerebral blood flow, its improvement of heart performance, of the metabolism of the brain, and because it is well toleraded. Different routes of synthesis are discussed.
The tritiation of (+)-(R)-alpha-((S)-1-[(3,3-di-3-thienylallyl)amino]-ethyl)-benzylalcohol (tinofedrine) is reported. The introduction of tritium was effected by partial hydrogenation of propiolic acid ester to the corresponding tritiated acrylic ester.
With the aid of spectroscopical methods the structure of (+)-(R)-alpha-[(S)-1-[(3,3-di-3-thienylallyl)amino]-ethyl]-benzyl-alcohol (tinofedrine, 1), a new cerebrally active compound, was confirmed. The relative and absolute configuration is discussed in view of spectroscopic data.
Different dianisyl-pyridyl- and dipyridyl-anisyl-methanoles react with sulfuric acid, hydrogen iodide or formic acid. Depending on the position of the methoxy groups, pyridine nucleus and acid demethylation or reduction occurs and 10-aryl-pyridol[1,2-alpha]-indole or 9-pyridyl-xanthenole-9, respectively, are formed as main or byproduct. UV-, IR- and 1H-NMR-spectra of the pyridonindoles are discussed.
The synthesis of tinofedrine (I), (+)-(R)-alpha-((S)-1-[3,3-di-3-thienylallyl)amino]benzylalcohol, a new cerebrally active drug, and the verification of its structure by spectrometric methods are reported.
Explore the source record for details and available documents.