A Practical Synthesis of Multitargeted Antifolate LY231514

Author:

Barnett Charles J.1,Wilson Thomas M.1,Kobierski Michael E.1

Affiliation:

1. Chemical Process Research and Development Division, Lilly Research Laboratories, a division of Eli Lilly and Company, Indianapolis, Indiana 46285-4813

Publisher

American Chemical Society (ACS)

Subject

Organic Chemistry,Physical and Theoretical Chemistry

Reference13 articles.

1. The renewed potential for folate antagonists in contemporary cancer chemotherapy

2. A dideazatetrahydrofolate analog lacking a chiral center at C-6: N-[4-[2-(2-amino-3,4-dihydro-4-oxo-7H-pyrrolo[2,3-d]pyrimidin-5yl)ethyl[benzoyl]-L-glutamic acid is an inhibitor of thymidylate synthase

3. A preliminary report of this work has been published:  Barnett, C. J.; Wilson, T. M.; Kobierski, M. E. InChemistry and Biology of Pteridines andFolates1997; Pfleiderer, W., Rokos, H., Eds.; Blackwell Wissenschafts-Verlag:  Berlin, 1997; pp 123−126.

4. A convenient method for regioselective C-5 halogenation of 4(3H)-oxo-7H-pyrrolo[2,3-d]pyrimidines

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