Synthesis of the immunosuppressive agent 2-morpholinoethyl mycophenolate by a lipase-catalyzed transesterification |
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Authors: | Patrizia Ferraboschi Paride Grisenti Daniele Pengo Paolo Prestileo |
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Abstract: | The synthesis of 2-morpholinoethyl mycophenolate was realized by an enzymatic transesterification of simple esters of mycophenolic acid with 2-morpholinoethanol. Best results were achieved by a Candida antarctica lipase B (CAL B) catalyzed transesterification of ethyl mycophenolate in toluene. CAL B showed to selectively transform only the ethyl ester function leaving unreacted the other functional groups present on the substrate. By this way 2-morpholinoethyl mycophenolate was obtained in satisfactory yields from mycophenolic acid (84%). |
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Keywords: | biocatalyzed transesterification Candida antarctica lipase B immunosuppressant mycophenolate mofetil |
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