Application of 77925-80-5, A common heterocyclic compound, 77925-80-5, name is N-(Benzyloxy)-2-nitrobenzenesulfonamide, molecular formula is C13H12N2O5S, 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.
2S,5S)-1-(tert-butyl) 2-ethyl 5-hydroxylpiperidine-1,2-dicarboxylate (130 g, 475.62 mmol), triphenylphosphine (212 g, 809.16 mmol) and N-(benzyloxy)-2-nitrophenyl-1-sulfamide (161.4 g, 523.5 mmol) were dissolved in tetrahydrofuran (1500 mL), cooled to 0C, diethyl azodicarboxylate (149.1 g, 856.16 mmol) was added dropwise under nitrogen gas protection, after adding, the reaction solution was heated to room temperature and stirred overnight, concentrated, and the crude product was purified by silica gel chromatograph (ethyl acetate : petroleum ether = 1:5) to obtain the title compound as a yellow oil (210 g, yield 78%).
The synthetic route of 77925-80-5 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; Xuanzhu Pharma Co., Ltd.; WU, Frank; (77 pag.)EP3281942; (2018); A1;,
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