Aliskiren is a direct renin inhibitor. Its indication is essential (primary) hypertension.
Synthetic Routes
Aliskiren route 1
Synthetic Reference
A convergent synthesis of the renin inhibitor CGP60536B; Sandham, D. A.; Taylor, R. J.; Carey, J. S.; Fassler, A.; Tetrahedron Letters; Volume 41; Issue 51; Pages 10091-10094; Journal; 2000
Aliskiren route 2
Synthetic Reference
A convergent synthesis approach towards CGP60536B, a non-peptide orally potent renin inhibitor, via an enantiomerically pure keto lactone intermediate; Rueger, H.; Stutz, S.; Goschke, R.; Spindler, F.; Maibaum, J.; Tetrahedron Letters; Volume 41; Issue 51; Pages 10085-10089; Journal; 2000
Process for the preparation of substituted octanoyl amides utilizing a stereoselective halolactonization; Herold, Peter; Stutz, Stefan; Spindler, Felix; Assignee Speedel Pharma Ag, Switz.; 2002; Patent Information; Jan 10, 2002; WO 2002002508 A1
Aliskiren route 5
Synthetic Reference
Convergent Synthesis of the Renin Inhibitor Aliskiren Based on C5-C6 Disconnection and CO2H-NH2 Equivalence; Cini, Elena; Banfi, Luca; Barreca, Giuseppe; Carcone, Luca; Malpezzi, Luciana; Manetti, Fabrizio; Marras, Giovanni; Rasparini, Marcello; Riva, Renata; Roseblade, Stephen; Russo, Adele; Taddei, Maurizio; Vitale, Romina; Zanotti-Gerosa, Antonio; Organic Process Research & Development; Volume 20; Issue 2; Pages 270-283; Journal; 2016