Provided herein are compounds of formula (V) that bind to BF3 of an androgen receptor (AR), which can modulate the AR for the treatment of Kennedy's disease.
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Page/Page column 40; 131
(2022/02/05)
Synthesis of 5-Trifluoromethyl-Substituted (Z)- N, N -Dimethyl- N '-(pyrazin-2-yl)formimidamides from 2-Aminopyrazines, LiI/Selectfluor, FSO 2CF 2CO 2Me and DMF under Cu Catalysis
The synthesis of 5-trifluoromethyl-substituted (Z)-N,N-dimethyl-N'-(pyrazin-2-yl)formimidamides via the iodination of 2-aminopyrazines with Selectfluor/LiI followed by a domino trifluoromethylation with FSO2CF2CO2Me and a condensation with DMF in the presence of CuI is realized under mild conditions. This three-step method offers CF3-substituted (Z)-N,N-dimethyl-N'-(pyrazin-2-yl)formimidamides in yields of 55 70% and with high regioselectivities. LiI serves as an iodine source, whilst DMF functions as both a solvent and a condensation reagent. The regioselectivity of these trifluoromethylation reactions is strongly dependent upon the substituent pattern on the 2-aminopyrazines. A possible mechanism for this method is also discussed.
A number of monosubstituted pyrazines, pyrimidines, and their N-oxides having the electron-donating amino groups were successfully iodinated.Depending on the reaction conditions, the 3-substituted pyrazine 1-oxides having a bulky dialkylamino group yielded the 6-iodo and 2,6-diiodopyrazine N-oxide derivatives together with some deoxygenated products.The mechanism with supportive evidence was presented to account for these chemical transformations.
Jovanovic, Misa V.
p. 1195 - 1210
(2007/10/02)
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