ChemInform Abstract: Synthesis and Biological Activity of 5‐Fluoroalkylthio‐6‐azauridines.

Abstract

The azauracils (I) are transformed into the azauridines (VII) and (VIII) via the silyl ethers (IV).

Copper‐Mediated Trifluoromethylthiolation of Heteroaryl Bromides

“…[1] Fore xample, these compounds can be found in insecticides [2] as well as anti-inflammatory, [3] and anticoccidial agents [4] (Scheme 1). [1] Fore xample, these compounds can be found in insecticides [2] as well as anti-inflammatory, [3] and anticoccidial agents [4] (Scheme 1).…”

“…Compounds containing the (trifluoromethyl)thio group (SCF 3 ) are extremely useful scaffolds in the pharmaceutical, agricultural, and advanced materials industries, mainly due to the high electron‐withdrawing effect and useful lipophilicity (π R =1.44) of the SCF 3 group 1. For example, these compounds can be found in insecticides2 as well as anti‐inflammatory,3 and anticoccidial agents4 (Scheme ). The development of efficient procedures for the introduction of a SCF 3 group into organic compounds is therefore of considerable interest 5…”

“…entries[2][3][4][5][6][7][8]. Other solvents, such as DMF,N MP,t oluene,and THF gavelower reactivity (Table 1, entries 2, and 4-6), whereas DMSO provided less interesting results (Table 1, entry 3).…”