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Reagents and Conditions: (a) Formaldehyde in THF, DBU, 0 °C to rt, 2 h; (b) HCl, MeOH, rt, 1 h, 6% for two steps; (c) Et3N, acetyl chloride, DCM, rt, 12 h; then HCl, MeOH, rt, 1 h, 3% for three steps; (d) K2CO3, CH3I, DMF, rt, 6 h; then HCl, MeOH, rt, 1 h, 4% for three steps; (e) Formaldehyde in THF, DBU, 0 °C to rt, 2 h, 42%; (f) Compound 13, Et3N, DCM, rt, 12 h; and (g) HCl, MeOH, 1 h, 7% for two steps.
