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A facile synthesis of 3-aryl pyroglutamic acid. Facile synthesis of baclofen and chlorpheg |
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| Authors: | Meng-Yang ChangPei-Pei Sun Shui-Tein Chen Nein-Chen Chang |
| Affiliation: | a Institute of Biological Chemistry, Academia Sinica, Nankang, Taipei 115, Taiwan b Department of Chemistry, National Sun Yat-Sen University, Kaohsiung 804, Taiwan |
| Abstract: | A facile synthesis of 3-aryl pyroglutamic acids via stepwise [3+2] annulation and desulfonated hydrolysis is reported. Base-induced coupling/cyclization reactions of α-sulfonylacetamide with various β-functional groups of (Z)-2-bromoacrylates yielded three contiguous chiral centers on the polysubstituted pyroglutamates system with trans-trans orientation in a one-pot synthesis. This facile strategy was used to synthesize amino acid derivatives baclofen and chlorpheg. |
| Keywords: | glutarimides stepwise [3+2] annulation baclofen chlorpheg pyroglutamic acid |
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