Efficient Synthesis and Practical Resolution of 1-(Naphthalen-1-yl) ethanamine, a Key Intermediate for Cinacalcet

…, SS Ippar, NC Niphade, RK Panchangam…

文献索引：Mathad, Vijayavitthal T.; Shinde, Gorakshanath B.; Ippar, Sharad S.; Niphade, Navnath C.; Panchangam, Raghavendra K.; Vankawala, Pravinchandra J. Synthetic Communications, 2011 ,  vol. 41,  # 3  p. 341 - 346

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被引用次数: 2

摘要

An efficient synthesis of 1-(naphthalen-1-yl) ethanamine (RS-2) and its practical resolution to optically pure (1 R)-(naphthalen-1-yl) ethanamine (R-(+)-2), a key intermediate in the synthesis of cinacalcet hydrochloride (1), is described. The resolution of RS-2 using R-(−)- mandelic acid as a resolving agent in ethanol was established on an industrial scale to give pure R-(+)-2 with> 99.8% ee after liberation of the amine from its mandelate salt. An ...