- SYNTHESIS OF ACYLOXYALKYL CARBAMATE PRODRUGS AND INTERMEDIATES THEREOF
-
Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.
- -
-
Page/Page column 40
(2008/06/13)
-
- Aryloxymethylcarbonochloridate ester intermediates for use in synthesizing pro drugs and their use therefor
-
The present invention relates to hitherto unknown intermediate of formula, in which R1 stands for hydrogen or a straight or branched aliphatic C1 -C20 carbon chain or an aryl or aralkyl group, aryl and "ar" meaning an aromatic or heterocyclic, 5- or 6-membered ring substituent containing 1 or 2 hetero atoms selected among O, S and N, R1 optionally being further substituted, and its chain being interrupted by hetero atoms like oxygen, or by carbonyl group(s); and R3 stands for hydrogen or C1 -C3 alkyl. The present intermediates can be used in a one step method for producing prodrugs of formula, where D-H =drug itself.
- -
-
-