Synthesis of labelled N‐(4‐hydroxy‐[14C(U)]phenyl)‐2‐[2,3‐dihydro‐3‐oxo‐l,2‐benzisothiazol‐2‐yl‐1,1‐dioxide]acetamide |
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Abstract: | The amidation of 2‐[1,1‐dioxide‐3‐oxo‐1,2‐benzisothiazole‐2(3H)‐yl] acetyl chloride with carbon‐14‐labelled 4‐amino‐[14C(U)]phenol in NaOAc‐HOAc buffer solution at ?10°C gave N‐(4‐hydroxy‐[14C(U)]phenyl)‐2‐[2,3‐dihydro‐3‐oxo‐1,2‐benziso‐thiazol‐2‐yl‐1,1‐dioxide]acetamide in 82% yield. Subsequent hydrolysis with aqueous 0.5 N NaOH solution afforded the ring opened product N‐(4‐hydroxy‐[14C(U)]‐phenyl)‐2‐[2‐carboxy‐phenylsulfonamido]acetamide in 80% yield. Copyright © 2005 John Wiley & Sons, Ltd. |
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Keywords: | analgesic anti‐pyretic acetaminophen carbon‐14 |
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