초록

A new class of nucleoside phosphoramidites which are relatively stable to permit isolation thereof and storage at room temperature. The phosphoramidites are derivatives of saturated secondary amines.

대표청구항 ▼

In a process for producing oligonucleotides which comprises the step of condensing the 3′-OH or 5′-OH group of a nucleoside or oligonucleotide with a nucleoside phosphite, the improvement being that the nucleoside phosphite is a compound of one of the formulae: [Figure] wherein B is a nucleoside or

In a process for producing oligonucleotides which comprises the step of condensing the 3′-OH or 5′-OH group of a nucleoside or oligonucleotide with a nucleoside phosphite, the improvement being that the nucleoside phosphite is a compound of one of the formulae: [Figure] wherein B is a nucleoside or deoxynucleoside base; A is H OH or OR4 in which R4 is a blocking group; R is a blocking group; R1′is a hydrocarbyl radical containing up to about carbon atoms; and X is NR2′R3′, wherein R2′and R3′taken separately each represent alkyl, aryl, aralkyl, cycloalkyl and cycloalkylalkyl containing up to 10 carbon atoms; R2′and R3′when taken together form an alkylene chain containing up to 5 carbon atoms in the principal chain and a total of up to 10 carbon atoms with both terminal valence bonds of said chain being attached to the nitrogen atom to which R2′and R3′are attached; and R2′and R3′when taken together with the nitrogen atom to which they are attached form a saturated nitrogen heterocycle including at least one additional heteroatom from the group consisting of nitrogen, oxygen and sulfur.