Patent ID: 6797819
Filing Date: 2004-09-28
Classification: C07B,C07D,C40B

Abstract:
A compound having the structure (I): wherein R1 is hydrogen or halogen, or is an aliphatic, heteroaliphatic, aryl, heteroaryl, alkylaryl, alkylheteroaryl moiety or is SRA, N(RA)2, or ORA, wherein RA is hydrogen or is an aliphatic, heteroaliphatic, aryl, heteroaryl, alkylaryl, or alkylheteroaryl moiety; R2 is hydrogen or is an aliphatic, heteroaliphatic, aryl, heteroaryl, alkylaryl, or alkylheteroaryl moiety R2 is a solid support optionally attached through a linker moiety; R3 is hydrogen or is an aliphatic, heteroaliphatic, aryl, heteroaryl, alkylaryl, alkylheteroaryl moiety or wherein R3 is â€”CN; â€”O(CN)Rx; â€”C(O)Rx; â€”CO2(Rx); â€”CON(Rx)2; â€”OC(O)Rx; â€”OCO2Rx; â€”OCON(Rx)2; â€”N(Rx)2; â€”S(O)2Rx; wherein each occurrence of Rx is independently hydrogen, aliphatic, heteroaliphatic, aryl, heteroaryl, alkylaryl, or alkylheteroaryl; R4 is hydrogen or is an aliphatic, heteroaliphatic, aryl, heteroaryl, alkylaryl, alkylheteroaryl moiety; R5 is hydrogen, halogen, â€”NO2, â€”CN, â€”C(O)Rx, â€”CO2(Rx), â€”CON(Rx)2, â€”OC(O)Rx, â€”OCO2Rx, â€”OCON(Rx)2, â€”N(Rx)2, â€”S(O)2Rx, wherein each occurrence of Rx independently includes aliphatic, heteroaliphatic, aryl, heteroaryl, alkylaryl, or alkylheteroaryl; or R5 is an aliphatic heteroaliphatic, aryl, heteroaryl, alkylaryl, alkylheteroaryl moiety, or is SRA, N(RA)2, or ORA, wherein RA is an aliphatic, heteroaliphatic, aryl, heteroaryl, alkylaryl, or alkylheteroaryl moiety; X is O, S or NR6, wherein R6 is OR7, NHR7, or NH(S(&boxH;O)2)R7, wherein R7 is aliphatic, heteroaliphatic, aryl, heteroaryl, alkylaryl, or alkylheteroaryl; and wherein each of the foregoing aliphatic, heteroaliphatic, alkylaryl, or alkylheteroaryl moieties may be cyclic or acyclic, and linear or branched; and each of the foregoing aliphatic, heteroaliphatic, aryl, heteroaryl alkylaryl, or alkylheteroaryl moieties may be unsubstituted or substituted with one or more substituents independently selected from the group consisting of aliphatic; heteroaliphatic; aryl; heteroaryl; alkylaryl; alkylheteroaryl; alkoxy; aryloxy; heteroalkoxy; heteroaryloxy; alkylthio; arylthio; heteroalkylthio; heteroarylthio; F; Cl; Br; I; â€”OH; â€”NO2; â€”CN; â€”CF3; â€”CH2CF3; â€”CHCl2; â€”CH2OH; â€”CH2CH2OH; â€”CH2NH2; â€”CH2SO2CH3; â€”C(O)Rx; â€”CO2(Ry); â€”CON(Ry)2; â€”OC(O)Ry; â€”OCO2Ry; â€”OCON(Ry)2; and â€”S(O)2)Ry; wherein each occurrence of Ry independently includes aliphatic, heteroaliphatic, aryl, heteroaryl alkylaryl, or alkylheteroaryl; and wherein the dotted line indicates the absence of a bond or indicates a bond, whereby a single bond or double bond is present, respectively.