With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.111769-27-8,(R)-Tetrahydrofuran-3-amine 4-methylbenzenesulfonate,as a common compound, the synthetic route is as follows.
(R)-(+)-3-Aminotetrahydrofuran toluene-4-sulfonate (2.0 g, 7.7 mmol) was added to a suspension of (2S)-2-(4-bromophenyl)-4-((lR)-l-phenylethyl)morpholine (2.4 g, 6.9 mmol), palladium acetate (65 mg, 0.29 mmol), 2-(di-t-butylphosphino)biphenyl (170 mg, 0.57 mmol), and sodium tert-butoxide (3.4 g, 35.4 mmol) in tert-butanol (50 ml) at room temperature. After heating at 90 C for 6 hours, the resulting suspension was passed through a Celite column. The filtrate was concentrated under reduced pressure, and the residue was purified by silica gel chromatography eluting 5-10% methanol in chloroform to afford 4-((lR)-l-phenylethyl)-(2S)-2-(4-(N-((3R)-tetrahydrofuran-3-yl)amino)phenyl)morpholine (1.3 g, 53%) as white crystals. iH-NMR(CDCl3) 8 : 1.35 (3H, d, J=6.8 Hz), 2.04-2.16 (4H, m), 2.55-2.62 (lH, m), 3.08-3.12 (1H, m), 3.33-3.38 (lH, m), 3.67-3.93 (5H, m) ,3.98-4.02 (1H ,m) ,4.46-4.58 (2H ,m) ,6.57 (2H , d, J=7.2 Hz), 6.83 (lH, d, J=9.0 Hz), 7.21-7.33 (7H, m)
111769-27-8, As the paragraph descriping shows that 111769-27-8 is playing an increasingly important role.
Reference£º
Patent; MITSUBISHI PHARMA CORPORATION; SANOFI-AVENTIS; WO2006/28290; (2006); A1;,
Tetrahydrofuran – Wikipedia
Tetrahydrofuran | (CH2)3CH2O – PubChem