Journal of Organic Chemistry p. 1696 - 1701 (1993)
Update date:2022-08-04
Topics:
Miwa, Tetsuo
Hitaka, Takenori
Akimoto, Hiroshi
A novel and efficient synthetic method for the synthesis of pyrrolo<2,3-d>pyrimidine antifolates is described.The key reaction of this method is the photo-initiated free radical addition of bromomalononitrile or ethyl bromocyanoacetate to an enol ether to afford the backbone skeleton of the targeted antifolate molecule.The key intermediates 3 or 4 are smoothly converted to the pyrrolo<2,3-d>pyrimidine antifolates 1 or 2 in three steps and in high overall yield.
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