Application of 76308-26-4, A common heterocyclic compound, 76308-26-4, name is Ethyl 2-(trans-4-aminocyclohexyl)acetate hydrochloride, molecular formula is C10H20ClNO2, 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.
To a solution of cyclohexyl-[5-fluoro-2-((_R)-methoxy-phenyl-methyl)-benzoimidazol-l- yl] -acetic acid (350 mg, 0.88 mmol, 1.0 equiv) in DMF (5 mL) was added triethylamine (179 mg, 240 muL, 1.77 mmol, 2.0 equiv) and HATU (403 mg, 1.06 mmol, 1.2 equiv) and the mixture stirred at 40 0C. After 15 min, trans- (4-amino-cyclohexyl) -acetic acid ethyl ester hydrochloride (235 mg, 1.06 mmol, 1.2 equiv; [CAS RN 76308-26-4]) was added and stirring continued at 50 0C for 2 h. The solution was concentrated by evaporation under reduced pressure, the pH adjusted to 9 by addition of a solution of 1 M NaHCtheta3 and the aqueous layer extracted with dichloromethane. The combined organic phases were dried over MgStheta4 and concentrated by evaporation under reduced pressure. The crude material was used in the consecutive step without further purification. MS (ISP): 564.7 [M+H]+.
The synthetic route of 76308-26-4 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; F. HOFFMANN-LA ROCHE AG; BENSON, Gregory Martin; BLEICHER, Konrad; FENG, Song; GRETHER, Uwe; KUHN, Bernd; MARTIN, Rainer E.; PLANCHER, Jean-Marc; RICHTER, Hans; TAYLOR, Sven; WO2010/43513; (2010); A1;,
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