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US 4,757,141 AGranted
Amino-derivatized phosphite and phosphate linking agents, phosphoramidite precursors, and useful conjugates thereof
AssigneeApplied Biosystems, LLC
InventorsSteven Fung, Sam L. Woo, Lloyd M. Smith
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Abstract
The compounds of the invention include novel linking agents comprising 2-substituted-3-protected-1,3,2-oxazaphosphacycloalkanes and their phosphoramidite precursors. The compounds of the invention further include conjugates of the above linking agents with oligonucleotides and polymer supports. The compounds of the present invention are useful for linking organic moieties, such as fluorescent or chromogenic dyes, to polymer supports and oligonucleotides, particularly single- and double-stranded DNA and RNA fragments.
Claims17
A compound of the formula:
- ##STR9## wherein:
- i is 0 or 1;
- j is in the range of 2 to 10;
- k is 1 when i is 0, or k is 0 or 1 when i is 1;
- R.sub.1 is an amino protection group;
- R.sub.2 and R.sub.3 taken separately each represent hydrogen, lower alkyl, lower cycloalkyl, lower acyl, cyano, halo, or nitro;
- R.sub.4 is alkyl, alkenyl, aryl, aralkyl, or cycloalkyl containing up to 10 carbon atoms;
- and
- W represents a hydroxylic polymer support, or an oligonucleotide linked to a polymer support.
6 more elements
A compound of the formula:
- ##STR10## wherein:
- R.sub.1 is an amino protection group;
- s is in the range of 0 to 8, t is in the range of 0 to 8, and s+t is in the range of 1 to 8;
- R.sub.4 represents lower alkyl;
- electron-withdrawing beta-substituted ethyl;
- electron-electron-withrawing substituted phenyl;
- or electron-withdrawing substituted phenylethyl;
- i is O or l;
- k is l when i is O or k is O or l when i is l;
- and
- W is an oligonucleotide, a hydroxylic polymer support, or an oligonucleotide liked to a polymer support.
8 more elements
Dependencies are inferred from the claim text.