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A facile and improved route for the synthesis of the orally active spiroindoline-based growth hormone secretagogue,MK-677 was described.The key step adopted the Fischer indole/reduction strategy.The preparation of the key intermediates N-protected piperidine carboxaldehyde 5 and the N-Boc-O-benzyl-D-serine(2) are also optimized.
A facile and improved route for the synthesis of the orally active spiroindoline-based growth hormone secretagogue, MK-677 was described. Key step adopted the Fischer indole / reduction strategy. The preparation of the key intermediates N-protected piperidine carboxaldehyde 5 and the N-Boc-O-benzyl-D-serine (2) are also optimized.