Electric Literature of 42726-73-8,Some common heterocyclic compound, 42726-73-8, name is tert-Butyl methyl malonate, molecular formula is C8H14O4, 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 mixture of tert-butyl methyl malonate (31.1 g, 179 mmol) and magnesium chloride(17.02 g, 179 mmol) in 350 mL acetonitrile at 0°C is added triethylamine (100 mL, 715mmol). The mixture is stirred for 15 minutes at 0°C. 3-(benzyloxy)-4-oxo-4H-pyran-2-carbonyl chloride (43 g, 162 mmol) in acetonitrile (30 mL) is added dropwise. The reaction mixture is allowed to warm to room temperature and stirred for two hours. The reaction mixture is cooled to 0°C and quenched with 30 mL 6N HCI. To the resulting mixture is added 1 L ether and the mixture is transferred to a separatory funnel. The aqueous layer is removed and the organics are washed with 2 X 300 mL water followed by washings with brine until the ether layer is clear. The organic layer is dried over magnesium sulphate, filtered, then concentrated to give 1-(tert-butyl) 3-methyl 2-(3-(benzyloxy)-4-oxo- 4H-pyran-2-carbonyl)malonate which is used without further purification.
The synthetic route of 42726-73-8 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; NOVARTIS AG; JAIN, Rama; KOESTER, Dennis Christofer; MANNING, James R.; SUTTON, James Clifford; TAFT, Benjamin R.; WAN, Lifeng; ZHAO, Qian; (148 pag.)WO2017/153919; (2017); A1;,
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