Synthetic Route of 937046-98-5,Some common heterocyclic compound, 937046-98-5, name is 7-Bromopyrrolo[2,1-f][1,2,4]triazin-4-amine, molecular formula is C6H5BrN4, traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.
The bromopyrazole (prepared according to WO2009/132135) (0.5 g, 2.4 mmol) was suspended in anhydrous THF (10 mL) under N2(g). The suspension was stirred and TMSC1 (0.67 mL, 5.28 mmol) was added. The mixture was stirred for 20 min. at RT and then cooled to -78 C after which time a solution of n-BuLi (6 mL, 1.6 N in hexanes, 9.6 mmol) was added slowly. The reaction mixture was stirred for 10 min. at -78 C and then the lactone (1 g, 2.4 mmol) was added via syringe. When the reaction was complete as measured by LCMS, AcOH was added to quench the reaction. The mixture was concentrated under reduced pressure and the residue dissolved in a mixture of CH2C12 and H20 (100 mL, 1 :1). The organic layer was separated and washed with H20 (50 mL). The organic layer was then dried over anhydrous MgSC>4, filtered and concentrated under reduced pressure. The residue was subjected to silica gel chromatography eluting with0-50% EtOAc in hexanes to provide the product as a 1 :1 mixture of anomers (345 mg, 26% yield).LCMS m/z 553 [M+H].
The synthetic route of 937046-98-5 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; GILEAD SCIENCES, INC.; MACKMAN, Richard, L.; PARRISH, Jay, P.; RAY, Adrian, S.; THEODORE, Dorothy, Agnes; WO2012/12776; (2012); A1;,
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