US4816569A
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Nucleotide derivative
Assignee: Wakunaga Pharmaceutical Co Ltd
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Filing: 1985-10-30
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Granted: 1989-03-28
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Expires: 2005-10-30
Abstract
Abstract A nucleotide of the formula [IV] shown below: ##STR1## wherein: X is hydrogen or --CO--(CH 2 ) n --CO--R 3 ; each of m and n is an integer up to 20; R 0 is a protective group of a phosphoric acid group, R 1 is hydrogen or a protective group for a 5'-hydroxyl group, R 2 is hydrogen or a protective group for an amino group, R 3 is a carrier having an amino group as the functional group and bound at this functional group in this compound, Y is oxygen atom (--0--) or an imino group (--NH--). This nucleotide, when the X is --CO--(CH 2 ) n --CO--R 3 , has a carrier (R 3 ) through a spacer (--CO--(CH 2 ) m --CO--) on extension from the amino group of deoxycytidine and therefore can be used as the starting material, namely the resin, for synthesizing a 3'-aminated oligonucleotide according to the solid phase method.
Inventors
- 👤 Kenichi Miyoshi
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-06 17:38
CPC Classifications
C; C07; C07H; C07H19/00; C07H19/02; C07H19/04; C07H19/06; C07H19/10; C07H21/00; Y; Y02; Y02P; Y02P20/00; Y02P20/50; Y02P20/55
Claims Analysis
Total Claims: 17
Claim 1
Independent Claim
114 words
A nucleotide of the formula: ##STR3## wherein X is hydrogen or --CO(Ch 2 ) n --CO--R 3 ; wherein each of m and n is a natural number up to 20; and R o is selected from the group consisting of orthrochlorophenyl; para-chlorophenyl, phenylthio and 5'-chloro-8-oyquinoly; R 1 is hydrogen or a protective group of a 5'-end hydroxyl group selected from the group consisting of trityl, monomethoxy-trityl, di-methoxytrityl, and trimethyl acetyl and R 3 is an amino-lower alkylated polystyrene, an amino-lower alkylated silica gel or an aminated polyacrylomorpholide; and wherein R 2 is hydrogen or a protective group for an amino group; and Y is an oxygen atom (-0-) or an imino group (-NH-).
Claim 2
Dependent Claim
114 words
A nucleotide of the formula: ##STR3## wherein X is hydrogen or --CO(Ch 2 ) n --CO--R 3 ; wherein each of m and n is a natural number up to 20; and R o is selected from the group consisting of orthrochlorophenyl; para-chlorophenyl, phenylthio and 5'-chloro-8-oyquinoly; R 1 is hydrogen or a protective group of a 5'-end hydroxyl group selected from the group consisting of trityl, monomethoxy-trityl, di-methoxytrityl, and trimethyl acetyl and R 3 is an amino-lower alkylated polystyrene, an amino-lower alkylated silica gel or an aminated polyacrylomorpholide; and wherein R 2 is hydrogen or a protective group for an amino group; and Y is an oxygen atom (-0-) or an imino group (-NH-).
Claim 3
Dependent Claim
10 words
The nucleotide according to claim 1, wherein X is hydrogen.
Claim 4
Dependent Claim
14 words
The nucleotide according to claim 1, wherein X is --CO--(CH 2 ) n --CO--.
Claim 5
Dependent Claim
13 words
The nucleotide according to claim 1, wherein R 0 is an ortho-chlorophenyl group.
Claim 6
Dependent Claim
11 words
A nucleotide according to claim 1, wherein R 1 is hydrogen.
Claim 7
Dependent Claim
23 words
The nucleotide according to claim 1, wherein R 1 is a trityl group, a mono-methoxytrityl group, a di-methoxytrityl group, or a trimethylacetyl group.
Claim 8
Dependent Claim
13 words
The nucleotide according to claim 6, wherein R 1 is a dimethoxytrityl group.
Claim 9
Dependent Claim
11 words
A nucleotide according to claim 1, wherein R 2 is hydrogen.
Claim 10
Dependent Claim
17 words
A nucleotide according to claim 1, wherein R 2 is a trifluoroacetyl group or an ortho-nitrosulphenyl group.
Claim 11
Dependent Claim
13 words
The nucleotide according to claim 9, wherein R 2 is a trifluoroacetyl group.
Claim 12
Dependent Claim
21 words
The nucleotide according to claim 1, wherein R 3 is an amino-lower-alkylated polystyrene, an amino-lower-alkylated silica gel or an aminated polyacrylmorpholide.
Claim 13
Dependent Claim
15 words
The nucleotide according to claim 1, wherein m is an integer of 2 to 8.
Claim 14
Dependent Claim
15 words
The nucleotide according to claim 1, wherein n is an integer of 2 to 8.
Claim 15
Dependent Claim
113 words
A nucleotide of the formula: ##STR4## wherein X is hydrogen or --CO(CH 2 ) n --CO--R 3 ; wherein each of m and n is a natural number up to 20; and R o is selected from the group consisting of orthochlorophenyl, para-chlorophenyl, phenylthio and 5'-chloro-8-oxyquionolyl; R 1 is hydrogen or a protective group for a 5'-end hydroxyl group selected from the group consisting of trityl, monomethoxytrityl, di-methoxytrityl, and trimethylacetyl; and R 3 is an amino-lower alkylated polystryrene, an amino-lower alkylated silica gel or an aminated polyacrylmorpholide and wherein R 2 is hydrogen or a protective group for an amino group, and Y is an oxygen atom (-0-) or an imino group (-NH-).
Claim 16
Dependent Claim
113 words
A nucleotide of the formula: ##STR4## wherein X is hydrogen or --CO(CH 2 ) n --CO--R 3 ; wherein each of m and n is a natural number up to 20; and R o is selected from the group consisting of orthochlorophenyl, para-chlorophenyl, phenylthio and 5'-chloro-8-oxyquionolyl; R 1 is hydrogen or a protective group for a 5'-end hydroxyl group selected from the group consisting of trityl, monomethoxytrityl, di-methoxytrityl, and trimethylacetyl; and R 3 is an amino-lower alkylated polystryrene, an amino-lower alkylated silica gel or an aminated polyacrylmorpholide and wherein R 2 is hydrogen or a protective group for an amino group, and Y is an oxygen atom (-0-) or an imino group (-NH-).
Claim 17
Dependent Claim
24 words
The nucleotide according to claim 14, wherein said protective group for an amino group for R 2 is a trifluoroacetyl or an ortho-nitrosulfenyl group.
References Cited (Backward Citations)
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