Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof
View Patent ↗The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.
1. A compound of Formula (IV):
or a pharmaceutically acceptable salt thereof, wherein:
R 1 is methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl, tert-butyl, cyclobutyl, cyclopentyl, cyclohexyl, phenyl, benzyl or 3-pyridyl;
R 2 is methyl; and
R 3 is hydrogen.
2. The compound of claim 1 , wherein:
R 1 is methyl, ethyl, propyl, isopropyl or butyl;
R 2 is methyl; and
R 3 is hydrogen.
3. The compound of claim 1 , wherein:
R 1 is isopropyl;
R 2 is methyl; and
R 3 is hydrogen.