With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.76176-87-9,Thiomorpholine-1-oxide hydrochloride,as a common compound, the synthetic route is as follows.
To a solution of compound 1 (21.0 mg, 0.0467 mmol, 1.0 eq) in DMF (1 ml_) was added A/,A/-diisopropylethylamine (32.6 pL, 0.187 mmol, 4.0 eq), HATU (26.7 mg, 0.0701 mmol, 1.5 eq) and thiomorpholine-1 -oxide hydrochloride (2) (14.6 mg, 0.0935 mmol, 2.0 eq). The reaction was stirred at room temperature for 17.5 h then diluted with EtOAc (10 ml_), washed with 1 M HCI (2 x 10 ml_) and brine (10 ml_), dried over MgS04, filtered and concentrated in vacuo. Purification by silica gel chromatography using hexane/EtOAc/MeOH (1 :0:0 – 0:1 :0 – 0:9: 1 ) yielded compound FD as a white solid (17.6 mg, 68%). (1239) LCMS (ES): Found 550.9 [M+Hf. (1240) 1H NMR (300MHz, DMSO-cf6), d: 8.88 (d, J=1.3 Hz, 1 H), 8.45 (dd, J=2.6, 1.5 Hz, 1 H), 8.36 (d, J=2.6 Hz, 1 H), 7.85 (d, J=9.4 Hz, 1 H), 7.81 (d, J=9.4 Hz, 1 H), 7.75 (d, J=3.8 Hz, 1 H), 7.32 (d, J=3.8 Hz, 1 H), 5.72-5.80 (m, 2H), 4.34-4.48 (m, 1 H), 3.89-4.06 (m, 2H), 3.66-3.84 (m, 1 H), 2.75-3.1 1 (m, 4H). (1241) 19F NMR (282MHz, DMSO-cf6), d: -64.79 (s, 3F).
76176-87-9 Thiomorpholine-1-oxide hydrochloride 20441479, aThiomorpholine compound, is more and more widely used in various.
Reference£º
Patent; KARUS THERAPEUTICS LIMITED; SHUTTLEWORTH, Stephen Joseph; GATLAND, Alice Elizabeth; FINNEMORE, Daniel John; ALEXANDER, Rikki Peter; SILVA, Franck; CECIL, Alexander; (233 pag.)WO2019/166824; (2019); A1;,
Thiomorpholine – Wikipedia
Thiomorpholine | C4H9NS – PubChem