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. 2013 Feb 18;4(4):402–407. doi: 10.1021/ml300476v

Scheme 1. Synthesis of Fluorescent ρ1 GABAC Antagonists (S)-11a–g and (R)-11d.

Scheme 1

Reagents and conditions: (a) (S)-4-ACPBPA 6 or (R)-4-ACPBPA 7 [for (R)-10d], NaHCO3, water/DME/THF (1:1:0.3), room temperature for 16 h, 81–89%; (b) TFA/DCM (1:1), room temperature for 1–2 h, 92–98%; (c) NMA N-succinimidyl ester, NaHCO3, water/DME/THF (1:1:0.3), room temperature for 16 h, 75–84%.