Tetrahedron Letters

Synthesis of β-fluoro-β-proline

VS Yarmolchuk, PK Mykhailiuk, IV Komarov

Index: Yarmolchuk, Vladimir S.; Mykhailiuk, Pavel K.; Komarov, Igor V. Tetrahedron Letters, 2011 , vol. 52, # 12 p. 1300 - 1302

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Citation Number: 9

Abstract

Pyrrolidine 3-carboxylic acid, or β-proline (Fig. 1) is a constrained β-amino acid commonly used in the design of peptides with enhanced stability towards hydrolysis by proteases. 6 β-Proline is also a potent agonist of the strychnine-sensitive glycine receptor, 7 serves as a building block for the preparation of novel inhibitors of bacterial DNA gyrase 8 and forms the central moiety of a conformationally restricted, highly potent fibrinogen receptor antagonist. 9 In addition, ...