With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.88675-24-5,Tetrahydrofuran-3-amine,as a common compound, the synthetic route is as follows.
EXAMPLE 1 7,8-Dimethoxy-N-(tetrahydrofuran-3-yl)quinazolin-4-amine To a solution of 4-chloro-7,8-dimethoxyquinazoline (1.5 g, 6.7 mmol) in DMF (30 mL) was added tetrahydrofuran-3-amine (698 mg, 8.01 mmol), DIPEA (2.3 mL, 13 mmol). Nitrogen was bubbled through the mixture for 5 min. The reaction was then heated at 100¡ã C. for 2 h. The crude mixture was evaporated and the residue was dissolved in ethyl acetate (20 mL), and filtered. The solid was washed with ethyl acetate (10 mL) to give 7,8-dimethoxy-N-(tetrahydrofuran-3-yl)quinazolin-4-amine 1.4 g (76percent).The racemate of 7,8-dimethoxy-N-(tetrahydrofuran-3-yl)quinazolin-4-amine 1.4 g was purified by SFC separation and numbered according to the order of elution: [0117] Stereoisomer 1 (first eluting by SFC): 388 mg, [0118] LC-MS (m/z) 276.1 (MH+) tR (minutes, method 3)=1.82. [0119] [alpha]20D=?32 (c=0.10 mg/mL, MeOH) [0120] Stereoisomer 2 (second eluting by SFC): 413 mg [0121] LC-MS (m/z) 276.1 (MH+) tR (minutes, method 3)=1.81. [0122] [alpha]20D=23 (c=0.10 mg/mL, MeOH)
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Reference£º
Patent; Kehler, Jan; Rasmussen, Lars Kyhn; Langgard, Morten; US2015/175584; (2015); A1;,
Tetrahydrofuran – Wikipedia
Tetrahydrofuran | (CH2)3CH2O – PubChem