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Reagents and conditions: (a)595318.2a or 318.2b (3 equiv), NaOt-Bu (12 equiv), DMF, 100 °C, 15 min; (b)595318.2a (3 equiv), DMF, rt, 30 min; (c)595 NaOt-Bu (12 equiv), DMF, 100 °C, 10 min; (d)596318.2a or 318.2c (2.5 equiv), NaOt-Bu (10 equiv), DMF, 100 °C; (e)596 BAHA (6.0 equiv), DCM, rt, 10 min; (f)596 BAHA (6.0 equiv), DCM, rt, 15 min, then H2NNH2·H2O.
