## Abstract Synthesis of two tritiated 1α,25‐dihydroxy‐22‐oxavitamin D~3~ (OCT), [26‐^3^H~3~]OCT (3) and [2β‐^3^H]OCT (4), is described. [26‐^3^H~3~]OCT (3) was prepared by tritiation at the side chain with tritiated methylmagnesium iodide and [2β‐^3^H]OCT (4) was labeled at the A‐ring by tritiatio
Synthesis of 24-oxavitamin D3 and 1α-hydroxy-24-oxavitamin D3
✍ Scribed by Luis A. Sarandeses; María José Vallés; Luis Castedo; Antonio Mouriño
- Publisher
- Elsevier Science
- Year
- 1993
- Tongue
- French
- Weight
- 653 KB
- Volume
- 49
- Category
- Article
- ISSN
- 0040-4020
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✦ Synopsis
Couphng of the CD fragment, ketone 6 (obtamed by pamal synthesis from vitanun D2). either directly (Homer-Wmlg route) or via the denved enol mflate (dlenyne route) with the appropnate A-ring fragment, phosphme oxide amon 7 or enyne 10, 1s the key step m the syntheses of 24-oxavmunm D3 (ld) and la-hydroxy-24-oxavltamm D3 (le), respectrvely HO"
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A synthesis of 25hydroxy [23,24JH]vitamin D3 leading to a radiochemically pure product with a specific activity of 78 Wmmol is described. The structure of the product was confirmed by comparison with unlabeled material and its biological activity was established by in vitro conversion to la,25dihydr
Synthesis and Biological Evaluation of 1α,24-Dihydroxy-25nitrovitamin D 3 . -The synthesis of an active vitamin D 3 analogue (X), proceeding via palladium-catalyzed alkylative enyne reaction, is described. The corresponding 24(S)-isomer is found to be tenfold less potent than (X).