Methods for synthesis of prodrugs from 1-acyl-alkyl...

Chemistry: molecular biology and microbiology – Measuring or testing process involving enzymes or... – Involving urea or urease

Reexamination Certificate

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C532S001000, C546S157000, C548S309100, C548S332100, C560S024000, C560S033000, C560S148000

Reexamination Certificate

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06927036

ABSTRACT:
Disclosed is a method for synthesizing 1-(acyloxy)-alkyl derivatives of primary or secondary amine drugs from 1-acyl-alkyl derivatives of primary or secondary amine drugs, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amenable to scale-up. For example, 1-acyl-alkyl derivatives of gabapentin and pregabalin are oxidized to yield 1-(acyloxy)-alkyl derivatives of gabapentin and pregabalin, respectively.

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