9/6/21 News The origin of a common compound about 10203-58-4

The synthetic route of 10203-58-4 has been constantly updated, and we look forward to future research findings.

Reference of 10203-58-4,Some common heterocyclic compound, 10203-58-4, name is Diethyl isobutylmalonate, molecular formula is C11H20O4, 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 724: 2-(2-cyclopropylmethoxy-5-fluoro-4′-trifluoromethyl-biphenyl-4-yl)-4- methyl-pentanoic acid. Step lDiethyl 2-(2,5-difluoro-4-nitrophenyl)-2-isobutylmalonate2-Isobutylmalonic acid diethyl ester (40.Og, 0.185 mol) in DMF (5OmL) was added dropwise to a stirred suspension of sodium hydride (60% in mineral oil, 8.0g, 0.33 mol) in 200 mL DMF (20OmL) over 20 min. at O0C under nitrogen. The mixture was stirred for 0.5 h at room temperature, cooled to 0 C and l,2,4-trifluoro-5-nitro-benzene (30.0g, 169.5 mmol) in DMF (15OmL) was added dropwise. The resulting reaction mixture was stirred at room temperature for 16h, poured into ice water (20OmL) and extracted with EtOAc (3x10OmL). The combined organic phases were washed with water (3x10OmL), brine (10OmL) and dried (MgStheta4). Evaporation of solvent under reduced pressure gave a brown oil which was purified by column chromatography over silica gel (Heptane-EtOAc, gradient) to give 57.0 g (90%) of 2-(2,5- difluoro-4-nitrophenyl)-2-isobutylmalonic acid diethyl ester as yellow oil. H NMR (300 MHz, CDCVTMS): delta 7.87 (dd, J = 12.3, 6.0 Hz, IH), 7.79 (dd, J = 10.1, 6.4 Hz, IH), 4.30^1.18 (m, 4H), 2.27 (d, J = 5.8 Hz, 2H), 1.60-1.50 (m, IH), 1.26 (t, J = 7.1 Hz, 6H), 0.82 (d, J = 7.0 Hz, 6H); 13C NMR (75 MHz, CDCI3/TMS): delta 168.2, 155.1 (d, 1JcF = 252.3 Hz), 150.9 (d, 1JcF = 263.2 Hz), 135.7, 135.1, 120.0 (dd, 2JCF = 26.0, 3JCF = 4.0 Hz), 113.0 (d, 2JCF = 29.0 Hz), 62.3, 43.1, 24.9, 23.8, 13.8.

The synthetic route of 10203-58-4 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; ENVIVO PHARMACEUTICALS, INC.; WO2009/86277; (2009); A1;,
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