Patent ID: 7241882
Filing Date: 2007-07-10
Classification: A61P,C07H

Abstract:
1. A process for preparing a PNA derivative of Formula I wherein V is oxygen, sulfur, NR U is, independently of any other U, oxygen, sulfur or NH; u′ is, independently of any other u′, from 1 to 10; W is, independently of any other W, oxygen, sulfur or NR Y is, independently of any other Y, hydroxyl, mercapto, oxyanion, thioate or NR R R X is, independently of any other X, Z is hydroxyl, n is from 0 to 10; Q is hydroxyl, amino, NHR R and wherein {POLY} is described by the Formula II wherein {BLOCK} is, independently of any other {BLOCK}, described by Formula IIIA, wherein each building block {BLOCK} can be different, and wherein z′ is from 0 to 100; A is, independently of any other A, (CR B is, independently of any other B, D is, independently of any other D, (CR R wherein R and physiologically tolerated salts of the PNA derivative of the Formula I, with the proviso that at least one Y or Z radical is hydroxyl, mercapto, oxyanion or thioate; wherein said process comprises a) synthesizing a backbone for the PNA derivative, starting from the C terminus, by sequentially coupling with amidonucleic acid monomes, which are optionally N-terminally protected; b) optionally deprotecting the N-terminally protected PNA backbone; c) coupling a phosphorus (III) or a phosphorus (V) group to the N-terminus of the PNA backbone, using activated phosphorylating reagents optionally containing a spacer; d) optionally repeating step c); and e) optionally oxidizing the phosphorus (III) group to a phosphorus (V) group.