Lookup NU author(s): Professor Bernard Golding,
Professor Roger Griffin,
Dr Ian Hardcastle
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2- Morpholin4-yl-4-oxo-4H-chromen-8-yl2,2,2-trifluoromethanesulfonate is a key intermediate for the synthesis of the DNA-dependent protein kinase (DNA-PK) inhibitor 8-dibenzothiophen-4-yl-2-morpholin-4-yl-chromen-4-one(NU7441). Two improved methods for the synthesis of this triflate have been developed: (A) in 35% overall yield, through modification of the published route, and ( B) in 15% overall yield, by a new route employing a Baker - Venkataraman rearrangement to enable generation of the chromenone scaffold. Both syntheses depend on the judicious use of allyl protecting groups.
Author(s): Aristegui SR, El-Murr MD, Golding BT, Griffin RJ, Hardcastle IR
Publication type: Article
Publication status: Published
Journal: Organic Letters
Date deposited: 12/05/2010
ISSN (print): 1523-7060
ISSN (electronic): 1523-7052
PubMed id: 17165896
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