Electric Literature of 1535-73-5, A common heterocyclic compound, 1535-73-5, name is 3-Trifluoromethoxyaniline, molecular formula is C7H6F3NO, 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.
EXAMPLE 7; [5-(3-{4-[3-(Trifluoromethoxy)phenyllpiperazin-l-yl}isoxazol-5-yl)-2//-tetrazol-2-yllacetic acid; Step 1 : l-[3-(Trifluoromethoxy)phenvnpiperazine; A mixture of 3-(trifluoromethoxy)aniline (2.13 g, 12.0 mmol), bis(2- chloroethyl)amine hydrochloride (2.14 g, 12.00 mmol) and 2-(2-ethoxyethoxy)ethanol (3.0 mL) was heated at 160 °C for 6 h. After being cooled to room temperature, the mixture was poured into a 250 mL separatory funnel containing aqueous 1 N NaOH solution (100 mL) and extracted with MTBE (2 x 50 mL). The combined organic layers were washed with brine, dried over MgSO4, filtered and concentrated under reduced pressure. Purification by column chromatography through silica gel, eluting with 100percent CH2Cl2 to 80:20:3 CH2Cl2:EtOH:NH4OH, to afford the title compound as a light yellow oil. MS (ESI, Q+) m/z 247 (M + 1).
The synthetic route of 1535-73-5 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; MERCK FROSST CANADA LTD.; ISABEL, Elise; LACHANCE, Nicolas; LECLERC, Jean-Philippe; LEGER, Serge; OBALLA, Renata, M.; POWELL, David; RAMTOHUL, Yeeman, K.; ROY, Patrick; TRANMER, Geoffrey, K.; ASPIOTIS, Renee; LI, Lianhai; MARTINS, Evelyn; WO2010/94126; (2010); A1;,
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