These common heterocyclic compound, 6134-53-8, name is 4-Bromo-2,3-dihydro-1H-indene, 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. Quality Control of 4-Bromo-2,3-dihydro-1H-indene
A mixture of 4-bromoindane (60.0 mg, 304 umol), bis(pinacolato)diboron (92.7 mg, 365 umol), potassium acetate (59.7 mg, 608 umol) and Pd(dppf)Cl2 (11.1 mg, 15.2 umol) in dioxane (10 mL) was stirred at 90 C for 4 hrs under nitrogen. On completion, the reaction mixture was concentrated in vacuo. The residue was purified by silica gel chromatography (petroleum ether:ethyl acetate = 50:1) to give the title compound (50.0 mg, 57% yield) as a colorless oil.1H NMR (400MHz, CDCl3) delta = 7.60 (d, J = 7.2 Hz, 1H), 7.32 (d, J = 7.2 Hz, 1H), 7.14 (dd, J = 7.2, 7.2 Hz, 1H), 3.14 (t, J = 7.6 Hz, 2H), 2.90 (t, J = 7.6 Hz, 2H), 2.05 (m, 2H), 1.34 (s, 12H). (Intermediate C) 2-(1,3-Dihydroisobenzofuran-4-yl)-4,4,5,5-tetramethyl-1,3,2- dioxaborolane
The synthetic route of 4-Bromo-2,3-dihydro-1H-indene has been constantly updated, and we look forward to future research findings.
Reference:
Patent; RAZE THERAPEUTICS, INC.; MAINOLFI, Nello; (215 pag.)WO2018/106636; (2018); A1;,
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