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Synthesis of several isotopically labeled pyrrolo[1,3-d]pyrimidine analogs

✍ Scribed by John A. Easter; Wayne T. Stolle

Publisher
John Wiley and Sons
Year
2001
Tongue
French
Weight
143 KB
Volume
44
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

Four members of a novel class of pyrrolo[2,3‐d]pyrimidines that show potential for the treatment of asthma and neurodegenerative disorders, have been prepared with radioisotope labels and in one case with multiple stable isotope labels for ADME studies as part of the drug development process. The syntheses utilize an isotopically labeled 2,4,6‐trisubstituted pyrimidine as a common building block, readily prepared from isotopically labeled urea. Cyclizations of the pyrimidine with bromo‐ketones generate the ring fused pyrrolo[2,3‐d]‐pyrimidines with elegant efficiency as demonstrated by the preparation of structures 4, 5, 8 and 12. Copyright Β© 2001 John Wiley & Sons, Ltd.

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Synthesis of some pyrrolo[2,3-d]pyrimidi
Synthesis of some pyrrolo[2,3-d]pyrimidine and 1,2,3-triazole isonucleosides
✍ Ratnakar R. Talekar; Richard H. Wightman πŸ“‚ Article πŸ“… 1997 πŸ› Elsevier Science 🌐 French βš– 754 KB

Nucleoside analogues g, 9,10 and 11, in which a pyrrolo [2,3-d]pyrimidine ring is linked m a 2-hydmxymethyl-3-hydmxytetrahydroftwan, have been ~ The azide la used as an intermediate in the routm to Iitese COmlmun~ also gave access to the 1,2,3-triazole isonucleosides 12 and 13.