Synthetic Route of 110407-59-5, A common heterocyclic compound, 110407-59-5, name is 2-Chloro-4-fluorobromobenzene, molecular formula is C6H3BrClF, its 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.
To a solution of l-bromo-2-chloro-4-fluorobenzene (2.5 g, 12.0 mmol) in toluene (10 mL) at -70 C was added n-BuLi (1.6 M in hexane) (7.5 mL, 12.0 mmol) dropwise over 5 min by syringe along the wall of the flask. After adding, the reaction was stirred at this temperature for 30 min. Then the resulting solution was added into a solution of (S)- tert-butyl l,6-dioxohexahydropyrrolo[l,2-a]pyrazine-2(lH) -carboxylate (2.8 g, 10.9 mmol) in toulene (10 mL). After stirred at -70 C for 5 min, the reaction mixture was quenched with saturated NH4CI and extracted with EtOAc (2 x 20 mL). The organic layer was washed with brine, dried over Na2S04, filtered and concentrated in vacuo. The residue was purified by silica gel chromatography to give the title compound (850.0 mg, yield : 20%); m/z (ES+): 385 [M + H] + .
The synthetic route of 110407-59-5 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; LEO PHARMA A/S; BLADH, Haakon; FELDING, Jakob; ZHOU, Ding; CAI, Zhen-wei; SØRENSEN, Morten Dahl; WO2015/24878; (2015); A1;,
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