Diisopropylethylamine → 5-Bromo-N-[4-(4-tert-butylpiperazin-1-yl)phenyl][1,2,4]triazolo[1,5-a]pyrazin-8-amine

This compound may be prepared using methods as described for Compound 6, step 1, using 5,8-dibromo-[1,2,4]triazolo[1,5-a]pyrazine (0.308 g, 1.107 mmol), 4-(4-tert-butyl-piperazin-1-yl)-phenylamine (0.310 g, 1.33 mmol) and N-ethyldiisopropyl-amine (0.289 mL, 1.66 mmol) in 2-propanol (5 mL). The reaction mixture is partitioned between DCM and 1N NaOH, the organic layer is separated and washed with water and brine, dried over MgSO4, filtered and concentrated under vacuum. Trituration of the residue with diethyl ether and petroleum ether affords the title compound (440 mg, 92%) as a cream solid. LCMS: Rt 2.25 min (96%).

1. customThis compound may be prepared
2. customThe reaction mixture is partitioned between DCM and 1N NaOH
3. customthe organic layer is separated
4. washwashed with water and brine
5. dry with materialdried over MgSO4
6. filtrationfiltered
7. concentrationconcentrated under vacuum

ORD-Eintrag

ord-7122b2b843d94772af4a1fdbcd09863c

Quelldatensatz

uspto-grants-2011_03

DOI

10.6084/m9.figshare.5104873.v1

Patentnummer

US07915256B2