Application of 154350-29-5, These common heterocyclic compound, 154350-29-5, name is Cyclopropanesulfonamide, its 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.
A solution of compound 1-1 (0.52 g, 2.3 mmol), 2-(lH-7-azabenzotriazol-l-yl)- 1,1 ,3,3-tetramethyl uronium hexafluoro -phosphate methanaminium (HATU, 1.74 g, 4.6 mmol), and 4-dimethylaminopyridine (1.39 g, 1 1.6 mmol) in CH2CI2 (40 mL) was stirred at room temperature for 1 hour, followed by slow addition ofcyclopropanesulfonamide (0.57 g, 4.7 mmol), diisopropylethylamine (1.81 mL, 14.0 mmol), and l ,8-diazabicyclo[5,4,0]undec-7-ene (1.80 g, 11.7 mmol) over15 minutes. After the reaction mixture was stirred at room temperature overnight, the solvent was removed under vacuum. The residue was purified by silica gel column chromatography to give compound 1-2 (0.51 g, 66percent). MS m/z 353.1 (M++23); !H NMR (CDCI3) d 9.75 (brs, 1H), 5.64-5.51 (m, 1H), 5.30 (d, J = 17.4 H), 5.16 (d, J = 10.2 Hz, 1H), 2.95-2.89 (m, 1H), 2.19-2.10 (m, 1H), 1.93-1.88 (m, 1H), 1.47 (s, 9H), 1.46-1.38 (m, 1H), 1.32-1.23 (m, 2H), 1.15-1.00 (m, 2H).
The synthetic route of 154350-29-5 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; TAIGEN BIOTECHNOLOGY CO., LTD.; LIU, Chen-Fu; LEE, Kuang-Yuan; CHENG, Pei-Chin; LIU, Yo-Chin; LO, Pin; TSENG, Kuo-Feng; CHEN, Chih-Ming; KING, Chi-Hsin Richard; LIN, Chu-Chung; WO2011/34518; (2011); A1;,
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