Synthesis of the orally active spiroindoline-based growth hormone secretagogue, MK-677

Peter E. Maligres,Ioannis Houpis,Kai Rossen,Audrey Molina,Jess Sager,Veena Upadhyay,Kenneth M. Wells,Robert A. Reamer,Joseph E. Lynch,David Askin,R.P. Volante,Paul J. Reider,Peter Houghton

TETRAHEDRON（1997）

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摘要

The preparation of the Merck Growth Hormone Secretagogue; MK-677 is described. A Fischer indole/reduction based strategy provides the novel spiroindoline nucleus of this potent compound. This optimized sequence necessitates the isolation of only one intermediate 10 and provides MK-677 in 48% overall yield from isonipecotic acid 3. (C) 1997 Elsevier Science Ltd.

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关键词

Fischer indole,growth hormone secretagogue,MK-677,Rosenmund,spiroindoline

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