Synthesis

A new approach to the synthesis of the nonpeptide NOP receptor Antagonist J-113397

A Sulima, J Folk, AE Jacobson, KC Rice

Index: Sulima, Agnieszka; Folk, John; Jacobson, Arthur E.; Rice, Kenner C. Synthesis, 2007 , # 10 p. 1547 - 1553

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Citation Number: 4

Abstract

Abstract A new synthesis that eliminates the need for chromatographic separation in order to obtain multigram quantities of J-113397, a competitive antagonist of the N/OFQ-NOP receptor system, is reported. N-Benzyl protected 4-oxopiperidinecarboxylate was used as the starting material to obtain an N-benzyl intermediate that could be resolved at a relatively early stage in the synthesis. The crucial step in the synthesis was reduction of the double ...