A new synthetic route of trans-2-Aminocyclohexanol hydrochloride

At the same time, in my other blogs, there are other synthetic methods of this type of compound,5456-63-3, trans-2-Aminocyclohexanol hydrochloride, and friends who are interested can also refer to it.

With the rapid development and complex challenges of chemical substances, the synthesis of new drugs is usually one of the most effective ways to increase yield.5456-63-3, name is trans-2-Aminocyclohexanol hydrochloride, molecular formula is C6H14ClNO, molecular weight is 151.6345, as common compound, the synthetic route is as follows.Recommanded Product: 5456-63-3

a) 5-Bromo-N-((ilS,R,2RlS,)-2-hydroxy-cyclohexyl)-6-(2,2,2-trifluoro-ethoxy)-nicotinamide5-Bromo-6-(2,2,2-trifluoro-ethoxy)-nicotinic acid (75.0 g, 0.25 mol) was dissolved in DMF (850 mL). To the solution was added TBTU (91.0 g, 0.275 mol), N,N-diisopropylethyl amine (214 mL, 1.25 mol) and (7SR,2RS)-2-amino-cyclohexanol hydrochloride (41.7 g, 0.275 mol). The reaction mixture was stirred for 1.5 h at room temperature. The solvent wasevaporated in vacuo, the residue was partitioned between ethyl acetate (2500 mL) and 1 N sodium hydroxide solution (2000 mL), the water phase was separated, extracted once more with ethyl acetate (1000 mL) and the organic phases were washed 2 times with water (2×1500 mL). Organic phases were pooled, dried with MgS04 and concentrated to about 900 mL. The product precipitated upon stirring and cooling to 0C. Filtration, washing with ethyl acetate/n-heptane (1: 1) and drying in vacuo gave the title compound (81.1 g) as a white solid; MS (ISP) 397, 399 (M)+.

At the same time, in my other blogs, there are other synthetic methods of this type of compound,5456-63-3, trans-2-Aminocyclohexanol hydrochloride, and friends who are interested can also refer to it.

Reference:
Patent; F. HOFFMANN-LA ROCHE AG; ROEVER, Stephan; WRIGHT, Matthew; WO2011/29827; (2011); A1;,
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