CHRISTINA MARY JOSEPHINE FOX,MATTHEW DALE REEVES,DWIGHT D. WELLER,YONGFU LI.
申请号:
BRPI0819828
公开号:
BRPI0819828A2
申请日:
2008.11.14
申请国别(地区):
BR
年份:
2015
代理人:
摘要:
Morpholino compounds are provided having the structure (I): where R1 is selected from the group consisting of lower alkyl, di(lower alkyl)amino, and phenyl; R2 is selected from the group consisting of lower alkyl, monocyclic arylmethyl, and monocyclic (aryloxy)methyl; R3 is selected from the group consisting of triarylmethyl and hydrogen; and Y is selected from the group consisting of: a protected or unprotected hydroxyl or amino group; a chlorophosphoramidate group; and a phosphorodiamidate linkage to the ring nitrogen of a further morpholino compound or a morpholino oligomer. Such compounds include doubly protected morpholino guanine (MoG) monomers. Also described is their use in synthesis of morpholino oligomers, and further improved procedures for synthesis of morpholino oligomers, pertaining to deprotection of the protected morpholino ring nitrogen at each monomer coupling step.