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EP0090789A1 Expired / Lapsed EP ⏱️ 0.0 years remaining

Chemical DNA synthesis

Assignee: Monsanto Co
•
Filing: 1983-03-24
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Granted: —
•
Expires: 2003-03-24
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Abstract

Abstract A process for the production of oligonucleotides such as DNA is disclosed which comprises the phosphite triester method on inorganic solid support in which a hindered dialkylamino nucleoside phosphite having a total of 4 to 6 carbon atoms in the dialkyl group is employed as an intermediate reagent in the synthesis. The solid support preferably is controlled pore glass with a long spacer.

Inventors

  • 👤 Steven Paul Adams
  • 👤 Gerald Russell Galluppi

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-10-31 08:58
CPC Classifications
C; C07; C07H; C07H21/00

Claims Analysis

Total Claims: 24
Claim 1
Independent Claim 93 words
A process for the production of oligonucleotides which comprises the step of condensing the 5'-OH group of a nucleoside or oligonucleotide covalently linked to an inorganic solid support through the 3-0- linkage of said nucleosideor oligonucleotide with a hindered dialkylamino nucleoside phosphite of the following formula wherein B = protected purine or pyrimidine base, R = protecting group, R 1 + R 2 = alkyls in which the total number of carbon atoms is 4 to 6, R 3 = alkyl having one to 6 carbon atoms, and X = H or OR.
Claim 2
Dependent Claim 93 words
A process for the production of oligonucleotides which comprises the step of condensing the 5'-OH group of a nucleoside or oligonucleotide covalently linked to an inorganic solid support through the 3-0- linkage of said nucleosideor oligonucleotide with a hindered dialkylamino nucleoside phosphite of the following formula wherein B = protected purine or pyrimidine base, R = protecting group, R 1 + R 2 = alkyls in which the total number of carbon atoms is 4 to 6, R 3 = alkyl having one to 6 carbon atoms, and X = H or OR.
Claim 3
Dependent Claim 12 words
The process of Claim 1 in which the dialkylamino group is diethylamino.
Claim 4
Dependent Claim 12 words
The process of claim 1 in which the dialkylamino group is diisopropyl
Claim 5
Dependent Claim 12 words
The process of Claim 1 in which the dialkylamino group is methylisopropyl.
Claim 6
Dependent Claim 13 words
The process of Claim 1 in which R is a trityl protecting group.
Claim 7
Dependent Claim 13 words
The process of Claim 1 in which the inorganic solid support is silica.
Claim 8
Dependent Claim 15 words
The process of Claim 1 in which the inorganic solid support is controlled pore glass.
Claim 9
Dependent Claim 30 words
The process of Claim 1 in which the inorganic solid support is linked to nucleoside or oligonucleotide through a long chain spacer having at least 15 atoms in the chain.
Claim 10
Dependent Claim 34 words
The process of Claim 1 in which the dialkylamino group is diethyl and the inorganic solid support is controlled pore glass with a long chain spacer having at least 15 atoms in the chain.
Claim 11
Dependent Claim 34 words
The process of Claim 1 in which the dialkylamino group is diisopropyl and the inorganic solid support is controlled pore glass with a long chain spacer having at least 15 atoms in the chain.
Claim 12
Dependent Claim 34 words
The process of Claim 1 in which the dialkylamino group is methylisopropyl and the inorganic solid support is controlled pore glass with a long chain spacer having at least 15 atoms in the chain.
Claim 13
Dependent Claim 1 words
Diisopropylaminomethoxychlorophosphine.
Claim 14
Dependent Claim 1 words
Diisopropylaminomethoxychlorophosphine.
Claim 15
Dependent Claim 1 words
Methylisopropylaminomethoxychlorophosphine.
Claim 16
Dependent Claim 1 words
Methylisopropylaminomethoxychlorophosphine.
Claim 17
Dependent Claim 3 words
Diisopropylamino nucleoside phosphite.
Claim 18
Dependent Claim 3 words
Diisopropylamino nucleoside phosphite.
Claim 19
Dependent Claim 3 words
Methylisopropylamino nucleoside phosphite.
Claim 20
Dependent Claim 3 words
Methylisopropylamino nucleoside phosphite.
Claim 21
Dependent Claim 107 words
A process for the production of oligonucleotides which comprises the step of condensing the 5'-OH group of a nucleoside or oligonucleotide covalently linked to an inorganic solid support through the 3'-0- linkage of said nucleoside or oligonucleotide with a dialkylamino nucleoside phosphite of the following formula wherein B = protected purine or pyrimidine base, R = protecting group, R 1 , R 2 , and R 3 = alkyls having from one to 6 carbon atoms, X = H or OR, and in which the inorganic solid support is linked to nucleoside or oligonucleoside through a long chain spacer having at least 15 atoms in the chain.
Claim 22
Dependent Claim 107 words
A process for the production of oligonucleotides which comprises the step of condensing the 5'-OH group of a nucleoside or oligonucleotide covalently linked to an inorganic solid support through the 3'-0- linkage of said nucleoside or oligonucleotide with a dialkylamino nucleoside phosphite of the following formula wherein B = protected purine or pyrimidine base, R = protecting group, R 1 , R 2 , and R 3 = alkyls having from one to 6 carbon atoms, X = H or OR, and in which the inorganic solid support is linked to nucleoside or oligonucleoside through a long chain spacer having at least 15 atoms in the chain.
Claim 23
Dependent Claim 41 words
The process of Claim 1 in which the protecting group is a trityl group and in which detritylation of protected nucleoside residue is carried out by treatment with a protic acid having a pK of from about 1.2 to about 1.8.
Claim 24
Dependent Claim 19 words
The process of Claim 17 in which the protic acid is dichloroacetic acid having a pK of about 1.5.

References Cited (Backward Citations)

EP0035719A2 Cited
EP0061746A1 Cited

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