New downstream synthetic route of cis-4-Aminocyclohexanol hydrochloride

According to the analysis of related databases, 56239-26-0, the application of this compound in the production field has become more and more popular.

Reference of 56239-26-0, As we all know, there are many different methods for the synthesis of a compound, and people can choose the synthesis method that suits their own laboratory according to the actual situation. 56239-26-0, name is cis-4-Aminocyclohexanol hydrochloride, molecular formula is C6H14ClNO, The compound is widely used in many fields, so it is necessary to find a new synthetic route. The downstream synthesis method of this compound is introduced below.

To tert-butyl 3-(5-chloro-2-fluoropyridin-4-yl)phenyl((tetrahydro-2H-pyran-4- yl)methyl)carbamate (440 mg, 1.045 mmol) was added DMSO (4 ml), TEA (0.729 ml, 5.23 mmol), and (ls,4s)-4-aminocyclohexanol hydrochloride (476 mg, 3.14 mmol) . The reaction was stirred at 95-100 °C for 40 hr. The reaction was followed by LCMS. The reaction was let cool, added 250 ml of ethyl acetate, washed with saturated sodium bicarbonate, water (2x), filtered and concentrated to constant mass. The crude was purified by silica gel chromatography using 12g column eluting with 30-85percent ethyl acetate with heptane. The desired fractions were concentrated to constant mass, giving 363 mg of the titled compound as free base used without further purification. LCMS (m/z): 516.2 (MH+), rt = 0.80 min.

According to the analysis of related databases, 56239-26-0, the application of this compound in the production field has become more and more popular.

Reference:
Patent; NOVARTIS AG; ANTONIOS-MCCREA, William R.; BARSANTI, Paul A.; HU, Cheng; JIN, Xianming; MARTIN, Eric J.; PAN, Yue; PFISTER, Keith B.; SENDZIK, Martin; SUTTON, James; WAN, Lifeng; WO2012/66065; (2012); A1;,
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