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2005
Pyrrole derivatives
R 0120
4,5-Disubstituted cis-Pyrrolidinones as Inhibitors of 17β-Hydroxysteroid DehyII. Part 1. Synthetic Approach. — A novel approach to the title com25- 111 drogenase
pounds (V) is based on the base-promoted cyclization of alkynes (III) followed by
cis-selective catalytic hydrogenation of the resulting pyrrolinones. Product (Vc) is
transformed to inhibitor component (IX), a close analogue of the natural product
clausenamide. — (COOK*, J. H.; BARZYA, J.; BRENNAN, C.; LOWE, D.; WANG,
Y.; REDMAN, A.; SCOTT, W. J.; WOOD, J. E.; Tetrahedron Lett. 46 (2005) 9,
1525-1528; Dep. Chem. Res., Bayer Res. Cent., West Haven, CT 06516, USA; Eng.)
— Mais
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