Practical Synthesis of p??Aminophenethylspiperone (NAPS), a High??Affinity, Selective D2??Dopamine Receptor Antagonist

C Jin, LD Mayer, AH Lewin, KS Rehder…

文献索引：Jin, Chunyang; Mayer, Louise D.; Lewin, Anita H.; Rehder, Kenneth S.; Brine, George A. Synthetic Communications, 2008 , vol. 38, # 5 p. 816 - 823

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被引用次数: 1

摘要

Abstract Because attempts to scale up the published synthetic preparation of p?? aminophenethylspiperone (NAPS) by N??alkylation of spiperone with 4??nitrophenethyl bromide followed by reduction gave poor yields and difficulties during purification, an alternative synthetic approach has been developed. Use of 4??(N??tert??butyloxycarbonyl) aminophenethyl bromide to alkylate spiperone followed by the Boc group deprotection ...