# US 4,393,010 A · Nucleosidic phosphorylating agent and methods

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- Number: US 4,393,010 A
- Document ID: US4393010A
- Status: Granted
- Kind: A
- Application number: 06/294,689
- Filed: 1981-08-20
- Granted: 1983-07-12
- Earliest claimed: 1979-12-26
- Assignees: Genentech, Inc.
- Inventors: Roberto Crea
- Web page: https://patentgrep.com/patent/US4393010A

## CPC

- C07H 21/00: Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
- C07F 9/1406: {containing the structure Hal-P(=O)-O-aryl}
- Y02P 20/55: Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
- C07H: SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS (derivatives of aldonic or saccharic acids C07C, C07D; aldonic acids, saccharic acids C07C59/105, C07C59/285; cyanohydrins C07C255/16; glycals C07D; compounds of unknown constitution C07G; polysaccharides, derivatives thereof C08B; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification C12N15/00; sugar industry C13)
- C07F: ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM (metal-containing porphyrins C07D487/22)
- Y02P: CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS

## Abstract

Compounds of the formula ##STR1## where R is a base labile substituted-phenyloxy protecting group, are useful as phosphorylating reagents in the synthesis of oligonucleotides by a phosphotriester method.

## Claims

### Claim 1

A compound of structure ##STR8## where R is a base labile phenyloxy protecting group.

### Claim 2 (depends on 1)

A compound according to claim 1 wherein R is selected from the group consisting of p-chlorophenyloxy, o-chlorophenyloxy, 2,4-dichlorophenyloxy, p-nitrophenyloxy and p-methoxyphenyloxy groups.

### Claim 3

The compound of structure ##STR9##