Synthesis of Potential Purinoceptor Antagonists: Application of P1-tBu Phosphazene Base for Alkylation of Adenine in Solution and on Solid Phase.

Autor: Enkvist, Erki, Raidaru, Gerda, Uri, Asko, Patel, Roshni, Redick, Catherine, Boyer, JoséL., Subbi, Juhan, Tammiste, Indrek
Předmět:
Zdroj: Nucleosides, Nucleotides & Nucleic Acids; Feb2006, Vol. 25 Issue 2, p141-157, 17p, 4 Diagrams, 2 Charts
Abstrakt: Alkylation of adenine in solution and on solid phase was accelerated by phosphazene base P1-tBu compared to mineral bases. The reactions in solution afforded regioselectively the appropriate N9-alkylated adenines with high preparative yields while the reaction with polystyrene resin-bound N-bromoacetylated peptides gave three regioisomers (alkylated at the N9, N7, and N3 position of adenine) in a 4:2:1 molar ratio. Ten novel nonphosphate nucleotide analogues were tested in an ADP-induced platelet aggregation assay. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index
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