Synthesis and biological properties of (E)-5-(2-[82Br]bromovinyl)-1-(2-deoxy-2-fluoro-β-d-ribofuranosyl)uracil ([82Br]BVFRU)
✍ Scribed by Takashi Iwashina; Edward E. Knaus; Leonard I. Wiebe; Lihua Xu; D.Lorne Tyrrell; Dorothy R. Tovell
- Publisher
- Elsevier Science
- Year
- 1990
- Weight
- 370 KB
- Volume
- 41
- Category
- Article
- ISSN
- 0883-2889
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📜 SIMILAR VOLUMES
The reaction of [2-14C]-2 ,4-bis-O-(trimethylsilyl)uracil (2) with ~-~-acetyl-~-0-benzoyl-2-deoxy-2-fluoro-~-D-arabinofuranosyl bromide (3) yielded the 3-O-acety1-5-0-benzoyl nucleos e 4 which was hydrolyzed with methanolic ammonia to afford [ 2-feC]-T-( 2-deoxy-2fluoro-p-D-arabinofuranosy1)uracil (
The synthesis of t h e title canpound (7) is described. [2-14C] cytosine (I) is treated with an aqueous mixture of sodium bisulfite and sodium sulfate at 8OoC for 30 rnin. The resulting solid is then treated with aqueous sodiun hydroxide and passed through a cation exchange colunn, producing [ Z-14C
1-(2-Deoxy-2-fluoro-beta-D-ribofuranosyl-(E)-5-(2-iodovinyl)uracil (IVFRU) was coupled to a dihydropyridine <---> pyridinium salt redox chemical-delivery system (CDS) via a cleavable sugar-ester linkage as a site-directed approach to increase diffusion of the parent nucleoside into the central nervo