Synthesis of the immunosuppressive agent 2-morpholinoethyl mycophenolate by a lipase-catalyzed transesterification

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 show...

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Bibliographic Details
Published in:Biocatalysis and Biotransformation
Main Authors: P. Ferraboschi, P. Grisenti, D. Pengo, P. Prestileo
Format: Article in Journal/Newspaper
Language:English
Published: Taylor & Francis 2006
Subjects:
Biocatalyzed transesterification
Candida antarctica lipase B
Immunosuppressant
Mycophenolate mofetil
Settore BIO/10 - Biochimica
Antarc*
Antarctica
Online Access:http://hdl.handle.net/2434/24670
https://doi.org/10.1080/10242420500520975
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Summary: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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