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. 2012 Aug 22;3(10):823–827. doi: 10.1021/ml300186g

Scheme 1. Preparation of Anilinyl Piperazinyl Ureas: Variation of Benzyl Substituents.

Scheme 1

Reagents and conditions: (a) 1.1 mol equiv PhNCO, methylene chloride, 4 h, rt, 93%. (b) 4 N HCl in 1,4-dioxane, methylene chloride, 40 h, rt, 96%. (c) 1.5 mol equiv aldehyde (R defined in Table 1), 9 mol equiv diisopropylethylamine, 2.5 mol equiv MP-BH(OAc)3, THF, rt, 24 h, 17–66%.