5-Fluorouracil derivatives

Details 5-Fluorouracil derivatives 5-Fluorouracil derivatives

1976-09-28

1978-11-07

Coughlan, Jr., Paul M.

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

Organic compounds

Nitrogen attached directly or indirectly to the purine ring...

C07D23954

Patent

active

041247655

ABSTRACT:
5-Fluorouracil derivatives and a process for their preparation are provided. The 5-fluorouracil derivatives according to the invention have the general formula: ##STR1## R.sub.1 and R.sub.2 are the same or different and are hydrogen or ##STR2## with the proviso that both R.sub.1 and R.sub.2 are not hydrogen at the same time. A.sub.1, A.sub.2 and A.sub.3 are independently selected from hydrogen, and optionally substituted alkoxy and phenyloxy; at least one of A.sub.1, A.sub.2 and A.sub.3 being other than hydrogen. The 5-fluorouracil derivative is prepared by condensing 5-fluorouracil with a halide of the formula: ##STR3## in the presence of a base. The 5-fluorouracils according to the invention show anti-tumor activity.

REFERENCES:
patent: 3322526 (1967-05-01), Loux
patent: 3682917 (1972-08-01), Knuniants et al.
patent: 3912734 (1975-10-01), Giller et al.
patent: 3971784 (1976-07-01), Tada

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