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KMID : 0370220060500060393
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Yakhak Hoeji
2006 Volume.50 No. 6 p.393 ~ p.397
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Synthesis of 3-substituted 7-Halocephalosporanate Derivatives
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Koo Young-Jun
Song Jin-Won
Yim Chul-Bu
Im Chae-Uk
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Abstract
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The synthesis of new 3-substituted 7-halocephalosporanates was described. 7-ACA was reacted with thiols at pH 6.5~6.8 to affored the 3-substituted 7-ACA (1), which was treated with diphenyldiazomethane to give diphenylmethyl 7-aminocephalosporanate (2). The Halogenation of 7-aminocephalosporanate (2) with NaNO2, KBr, and H2SO4gave 7-bro-mocephalosporanate (3) and with NaNO2, HCl gave 7-chlorocephalosporanate (4). Diphenylmethyl cephalosporanate (2~4)were deprotected by AlCl3 in anisole and neutralized to give the sodium cephalosporanate (5~7).
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KEYWORD
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7-halocephalosporanate, B-lactamase inhibitors
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