Zusamnenfassung. 25-Hydroxycholestcrin (4) ist in 30proz. husbcute in sieben Schritten aus Stigmastcrin (6) hergestellt wordcn. Dcr wichtigste Schritt ist die Umsetzung des Tosylats 11 mit Clem hcctylenderivat 13 zu 14 unter Bildung d r s vollstandigen Cholesteringeriists. Significant breakthroughs have been made with respect to the structures and the modes of action of the biologically active forms of vitamin D, (1) [I]. 25-Hydroxycholecalciferol (2) [2] and 1 M , 25-dihydroxycliolecalciferol (3) [3], the major metabolites of cliolecalciferol (l), are inore potent than l in allthree criteriaof physiological activity, namely, increased calcium transport, bone mineral mobilization, and calcification [I]. Since hydroxylation occurs first in the liver (25-OH) and then in the kidney (3 cr.-OH) before the onset of activity [I], cholecalciferol (1) should be viewed 4 K -H 5 R = 01%
Das aus Stigmasterin und p‐Tosylchlorid in Pyridin erhaltene Tosylat (I) liefert beim Erhitzen mit Methanol neben Stigmasterylmethyläther überwiegend den Isostigmasteryläther (II), der in den Alkohol (IIIa) übergeführt wird.
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