The synthesis of 2-morpholinoethyl mycophenolate was realized by an enzymic 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 Et mycophenolate in toluene. CAL B showed to selectively transform only the Et 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%).
Synthesis of the immunosuppressive agent 2-morpholinoethyl mycophenolate by a lipase-catalyzed transesterification / P. Ferraboschi, P. Grisenti, D. Pengo, P. Prestileo. - In: BIOCATALYSIS AND BIOTRANSFORMATION. - ISSN 1024-2422. - 24:3(2006 May), pp. 209-213.
Synthesis of the immunosuppressive agent 2-morpholinoethyl mycophenolate by a lipase-catalyzed transesterification
P. FerraboschiPrimo
;
2006
Abstract
The synthesis of 2-morpholinoethyl mycophenolate was realized by an enzymic 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 Et mycophenolate in toluene. CAL B showed to selectively transform only the Et 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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