Tetrahedron

Crystallization-induced asymmetric transformation: Stereospecific synthesis of L-768,673

YJ Shi, KM Wells, PJ Pye, WB Choi, HRO Churchill…

文献索引：Shi, Yao-Jun; Wells, Kenneth M.; Pye, Philip J.; Choi, Woo-Baeg; Churchill, Hywyn R. O.; et al. Tetrahedron, 1999 , vol. 55, # 4 p. 909 - 918

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被引用次数: 17

摘要

A highly convergent, asymmetric synthesis of L-768,673, an Iks Class III antiarrythmic drug candidate, is described. Synthesis of the recemic 1-trifluoroethyl-3-amino-5-phenyl benzodiazepinone [(±)-amine] was achieved by Ru-catalyzed hydrogenation of the corresponding oxime that was derived from commercially available 1-trifluoroethyl-5-phenyl benzodiazepine in 76% overall yield. An efficient one-pot resolution-racemization of (±)- ...