Process for the preparation of fludarabine or fludarabine phosph

Details Process for the preparation of fludarabine or fludarabine phosph Process for the preparation of fludarabine or fludarabine phosph

1992-11-25

1997-02-11

Kunz, Gary L.

Organic compounds -- part of the class 532-570 series

Organic compounds

Carbohydrates or derivatives

536 263, 536 2761, 536 2763, C07H 100, C07H 19167, C07H 1920

Patent

active

056022468

ABSTRACT:
A process for the production of fludarabine or fludarabine phosphate is provided, wherein the nucleoside guanosine or a suitable derivative is employed as the starting material. The guanosine starting material is subjected to (a) conversion of the 6-keto group into a 6-amino group, (b) conversion of the 2-amino group to a 2-fluoro group, and (c) conversion of the ribofuranosyl moiety to an arabinofuranosyl moiety. Steps (a), (b), and (c) can be performed individually or concomitantly and in any sequence.

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