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Reagents and conditions: (i) R2R3NH2, Pd2dba3, Xantphos, K3PO4 or Cs2CO3, 1,4-dioxane, 100 °C or n-propylamine, CuI, 2-acetylcyclohexanone, K3PO4, DMF, 100 °C; (ii) LHMDS, THF then Boc2O or CbzCl; (iii) LDA, TMEDA, −78 °C, THF then 8, −78 °C to −20 °C or LHMDS, 8, THF, −78 °C to −20 °C; (iv) aqueous HF, CH3CN, or 1,4-dioxane; (v) 10% Pd/C, H2, HCl, MeOH, 1,4-dioxane; (vi) R2B(OH)2, (Ph3P)4Pd, K3PO4, toluene, 1,4-dioxane, H2O, 90 °C.
