公开(公告)号：US5175266A

公开(公告)日：1992-12-29

申请号：US687807

申请日：1991-04-19

申请人： Rajender S. Varma ,  Michael E. Hogan ,  Ganapathi R. Revankar ,  Takkellapati S. Rao

发明人： Rajender S. Varma ,  Michael E. Hogan ,  Ganapathi R. Revankar ,  Takkellapati S. Rao

IPC分类号： C07H19/06 ,  C07H19/16 ,  C12Q1/68

CPC分类号： C07H19/06 ,  C07H19/16 ,  C12Q1/6839

摘要： Nucleoside derivatives which contain a nucleo-base, a sugar and an amino acid backbone of the structure: ##STR1## where R' refers to the various amino acid side chains or their blocked equivalent and R refers to a nucleo-base or its blocked equivalent. The synthesis of these nucleoside derivatives proceeds by a series of steps including oxidation of the 3'-azido nucleoside derivative, coupling to a benzylated ester of an amino acid to yield the amide and hydrogenation. The adenine, guanine, cytosine and thymine nucleosides with an amino acid at the 5' terminus are synthesized. From such monomers oligonucleotides can be synthesized which possess an amino acid backbone, using either solid state phase chemistry or liquid phase chemistry.

摘要翻译： 含有核碱基，糖和氨基酸主链结构的核苷衍生物：其中R'表示各种氨基酸侧链或其封端的等同物，R指核碱基或其封闭的等同物 。 这些核苷衍生物的合成通过一系列步骤进行，包括3'-叠氮基核苷衍生物的氧化，与氨基酸的苄化酯偶联以产生酰胺和氢化。 合成具有5'末端氨基酸的腺嘌呤，鸟嘌呤，胞嘧啶核苷和胸腺嘧啶核苷。 从这样的单体可以使用固态相化学或液相化学合成具有氨基酸主链的寡核苷酸。