Patent ID: 6025482
Filing Date: 2000-02-15
Classification: A61K,C07D,C07F,C07H

Abstract:
A method for forming a covalent linkage having structure CH.dbd.N--R.sub.A --CH.sub.2, CH.sub.2 --R.sub.A --N.dbd.CH, or R.sub.A --N.dbd.CH--CH.sub.2 where R.sub.A is O or NR.sub.1, comprising the steps of:(a) providing synthons having structure: ##STR4## (b) contacting said synthons for a time and under reaction conditions effective to form said covalent linkage;wherein:Z.sub.1 and Y.sub.2 are selected such that(i) Z.sub.1 is C(O)H and Y.sub.2 is CH.sub.2 R.sub.A NH.sub.2 ; or(ii) Z.sub.1 is CH.sub.2 R.sub.A NH.sub.2 and Y.sub.2 is C(O)H;(iii) Z.sub.1 is CH.sub.2 C(O)H and Y.sub.2 is R.sub.A NH.sub.2 ; or(iv) Z.sub.1 is R.sub.A NH.sub.2 and Y.sub.2 is H(O)CCH.sub.2 ;R.sub.1 and R.sub.2 are the same or different and are H; alkyl or substituted alkyl having 1 to about 10 carbon atoms; alkenyl or substituted alkenyl having 2 to about 10 carbon atoms; alkynyl or substituted alkynyl having 2 to about 10 carbon atoms; alkaryl, substituted alkaryl, aralkyl, or substituted aralkyl having 7 to about 14 carbon atoms; alicyclic; heterocyclic; a reporter molecule;B.sub.X1 and B.sub.X2 are, independently, nucleosidic bases;Q.sub.1 and Q.sub.2 are, independently, O, S, CH.sub.2, CHF or CF.sub.2 ; andX.sub.1 and X.sub.2 are, independently, H; OH; alkyl or substituted alkyl having 1 to about 10 carbon atoms; alkaryl, substituted alkaryl, aralkyl, or substituted aralkyl having 7 to about 14 carbon atoms; F; Cl; Br; CN; CF.sub.3 ; OCF.sub.3 ; OCN; O-alkyl; S-alkyl; N-alkyl; O-alkenyl; S-alkenyl; N-alkenyl; SOCH.sub.3 ; SO.sub.2 CH.sub.3 ; ONO.sub.2 ; NO.sub.2 ; N.sub.3 ; NH.sub.2 ; heterocycloalkyl; heterocycloalkaryl; aminoalkylamino; polyalkylamino or substituted silyl.