Phosphoramidites of the formula ##STR1## where R is a base-labile protecting group, R.sup.1 and R.sup.2 are individually alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 8 carbon atoms, or aryl of 6 to 20 carbon atoms or are joined together to form with the nitrogen atom a cyclic structure of 4-7 carbon atoms and 0 to 1 annular chalcogen atoms of atomic number 8 to 16, G is a hydrocarbylene group of 1 to 20 carbon atoms and Z is a hydroxy-protected vicinal diol group bound to G by one of the vicinal diol carbon atoms or a disulfide group and bound to G by one of the sulfur atoms of the disulfide group, with the proviso that G is of at least 4 carbon atoms when Z is said disulfide group are used in conventional automated oligonucleotide synthesis to introduce a functional aldehyde or thiol group on the 5' end of the oligonucleotide to thereby provide a reactive site on the oligonucleotide that may be used to conjugate the oligonucleotide to molecules that contain a free amino group or an electrophilic center reactive with a thiol group.
式子为##STR1##的
磷酰胺酯,其中R是一个碱性易去保护基,R1和R2分别为1到6个碳原子的烷基、3到8个碳原子的环烷基或6到20个碳原子的芳基,或与氮原子结合形成4-7个碳原子和0-1个原子序数为8到16的环
硫族原子的环状结构,G是1到20个碳原子的烃基,Z是通过邻二醇碳原子之一与G结合的羟基保护的邻二醇基团或通过二
硫键中的
硫原子之一与G结合的二
硫键基团,但前提是当使用Z为二
硫键基团时,G至少为4个碳原子。这些
磷酰胺酯可用于常规自动寡核苷酸合成,以在寡核苷酸的5'端引入一个功能性醛基或
硫醇基,从而在寡核苷酸上提供可用于将寡核苷酸与含有游离
氨基或与
硫醇基反应的亲电中心的分子结合的反应位点。