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

Authors
Rueger, H Stutz, S Goschke, R Spindler, F Maibaum, J
Citation
H. Rueger et al., A convergent synthesis approach towards CGP60536B, a non-peptide orally potent renin inhibitor, via an enantiomerically pure ketolactone intermediate, TETRAHEDR L, 41(51), 2000, pp. 10085-10089
Citations number
13
Categorie Soggetti
Chemistry & Analysis","Organic Chemistry/Polymer Science
Journal title
TETRAHEDRON LETTERS
ISSN journal
00404039 → ACNP
Volume
41
Issue
51
Year of publication
2000
Pages
10085 - 10089
Database
ISI
SICI code
0040-4039(200012)41:51<10085:ACSATC>2.0.ZU;2-8
Abstract
We report a convergent synthesis of the potent orally active non-peptide re nin inhibitor CGP60536B. The key reaction employs the coupling of the enant iopure Grignard species derived from chloride 13 with the diastereomericall y pure gamma -lactone 9b. The stereoselective reduction of the resulting ke tone 14b has been thoroughly investigated. (C) 2000 Elsevier Science Ltd. A ll rights reserved.