The synthesis of conformationally constrained analogues of the ACE inhibitor Idrapril
β Scribed by Iwan G Jones; Wyn Jones; Michael North
- Publisher
- Elsevier Science
- Year
- 1999
- Tongue
- French
- Weight
- 671 KB
- Volume
- 55
- Category
- Article
- ISSN
- 0040-4020
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β¦ Synopsis
A conformationally constrained analogue 3 of the ACE inhibitor Idrapril has been prepared by a five-step synthesis. The key step in the synthesis is the desymmetrization of endo-norbom-5-ene-2,3-dicarboxylic anhydride 4 by reaction with t-butyl (S)-prolinate.
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Conformationally constrained spirofuropyridine analogues of epibatidine, syn-2 and anti-2, in which the 7-azabicyclo[2.2.1]heptane system and the 2-chloropyridine ring are held rigidly with the shorter and longer N-N distances, respectively, were synthesized from N-Boc-7-azabicyclo[2.2.1]heptan-2-on
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