A convergent synthesis approach towards CGP60536B, a non-peptide orally potent renin inhibitor, via an enantiomerically pure ketolactone intermediate

✍ Scribed by Heinrich Rüeger; Stefan Stutz; Richard Göschke; Felix Spindler; Jürgen Maibaum

• Publisher: Elsevier Science
• Year: 2000
• Tongue: French
• Weight: 114 KB
• Volume: 41
• Category: Article
• ISSN: 0040-4039
• DOI: 10.1016/s0040-4039(00)01794-9

✦ Synopsis

We report a convergent synthesis of the potent orally active non-peptide renin inhibitor CGP60536B.

The key reaction employs the coupling of the enantiopure Grignard species derived from chloride 13 with the diastereomerically pure g-lactone 9b. The stereoselective reduction of the resulting ketone 14b has been thoroughly investigated.