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KMID : 0613820040140010091
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Journal of Life Science
2004 Volume.14 No. 1 p.91 ~ p.97
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Synthesis of N-acyl-α-aminosuccinimides and N-acyl-α-aminoglutarimides
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Jung Dai-Il
Kim Moon-Ju
Song Hyun-Ae
Lee Yong-Gyun
Park Yu-Mi
Park Min-Soo
Kim Yun-Young
Choi Soon-Kyu
Han Jung-Tae
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Abstract
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As a part of our study on the improvement of anticonvulsant, here we report the synthesis of N-acyl-α-aminosuccinimides 1 and N-acyl-α-aminoglutarimides 2. (R)-Benzoic acid 4-benzyloxycarbonylamino-2-oxo- pyrrolidin-1-ylester 6a, (R)-4-nitro-benzoic acid 4-benzyloxycarbonylamino-2- oxo-pyrrolidin-1-yl ester 6b, (R)-4-nitro-benzoic acid 4-benzyloxycarbonylamino-2-oxo-pyrrolidin-1-yl ester 6c, and (R)-propionic acid 4-benzyloxycarbonylamino-2-oxo-pyrrolidin-1-yl ester 6d were synthesized from (R)-2-benzyloxy carbonylamino-succinic acid 3 as a starting meterial. (R)-(3- Benzyloxycarbonylamino-2,6-dioxo- piperidin-1-yloxy)-acetic acid methyl ester 10a, (R)-(3-benzyloxycarbonylamino-2,6-dioxo-piperidin- 1-yloxy)-acetic acid ethyl ester 10b, and (R)-2-(3-benzyloxycarbonylamino-2,6-dioxo-piperidin-1-yloxy)- propionic acid methyl ester 10c were synthesized from (R)- 3-carbobenzyloxy-amino-glutarmic acid 7 as a starting meterial. The yield, mp, IR, ¹H-NMR, and 13C- NMR spectra of the products 6a, 6b, 6c, 6d, 10a, 10b, 10c are summarized in footnote. The biological studies of these compounds are in progress and will be reported in future.
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KEYWORD
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anticonvulsant, N-acyl-α-aminosuccinimides, N-acyl-α-aminoglutarimides, ME test, PTZ test
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