制备4-甲氧基-1-氧化吡啶-2-甲基N -2-(4,4'-二甲氧基三苯甲氧基)乙基-N-胸腺嘧啶-1-基-氨基甲基膦酸酯(1a,T ∗)和报道了相应的N 4-苯甲酰基胞嘧啶-1-基衍生物1b(C ∗)。这些PPNA单体被证明是固相合成十四聚体片段的基础材料(C * T * T * T * T * C * T * T * T * T * C * T *C ∗ T ∗)dT。
The invention provides conjugates that comprise a targeting moiety, a nucleic acid, and optional linking groups as well as synthetic intermediates and synthetic methods useful for preparing the conjugates. The conjugates are useful to target therapeutic nucleic acids to the liver and to treat liver diseases including hepatitis (e.g. hepatitis B and hepatitis D).
Novel synthetic routes to PNA monomers and PNA-DNA linker molecules
作者:Gerhard Breipohl、David W. Will、Anusch Peyman、Eugen Uhlmann
DOI:10.1016/s0040-4020(97)01044-2
日期:1997.10
Novel methods for the preparation of monomethoxytrityl (Mmt) protected aminoethylglycine building blocks and dimethoxytrityl (Dmt) protected hydroxyethylglycine derivatives useful for the synthesis of polyamidenucleicacids (PNAs) and PNA/DNA chimeras are described. The protecting group strategy employed for PNA monomer synthesis produces easily isolable intermediates, minimizes chromatographic purification