Chemoenzymatic synthesis of N-trifluoroacetyl doxorubicin-14-valerate (Valrubicin)

Organic Process Research and Development

Volumn 9, Issue 6, 2005, Pages 818-821

  Cotterill, Ian C ^a   Rich, Joseph O ^a,b  

^a ALBANY MOLECULAR RESEARCH INC   (United States)

^b NORTHWESTERN UNIVERSITY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

EID: 28944433323     PISSN: 10836160     EISSN: None     Source Type: Journal    
DOI: 10.1021/op0501186     Document Type: Article

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38. Given the relative cost of valeric acid and doxorubicin ($0.30/g and $90/g, respectively) on the research scale, a large (10-fold) molar excess of acid was employed in order to drive the esterification towards completion.
39. Initial findings (>95% residual activity remaining after five reaction cycles without any enzyme regeneration attempted) indicate that the enzyme is quite stable in the identified reaction system, and additional enzyme recycling could further reduce catalyst costs.