Patent US3875207A successfully refreshed from Google Patents.
US3875207A
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Process for the temporary protection of amino groups in peptide syntheses
Assignee: Novartis Corp
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Filing: 1972-03-30
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Granted: 1975-04-01
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Expires: 1992-03-30
Abstract
Abstract Temporary protection of amino groups by the group of the formula I in which R1 represents lower alkyl, R2 lower alkyl or phenyl and R3 phenyl, and wherein the phenyl radicals are unsubstituted or substituted by lower alkyl, phenyl or lower alkylphenyl groups.
Inventors
- 👤 Beat Iselin
- 👤 Peter Sieber
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-29 15:12
CPC Classifications
C; C07; C07K; C07K5/00; C07K5/04; C07K5/06; C07K5/06086; C07K1/00; C07K1/06; C07K1/061; C07K1/063; C07K1/064; C07K5/08; C07K5/0802; C07K5/0812; A; A61; A61K; A61K38/00
Claims Analysis
Total Claims: 20
Claim 1
Independent Claim
35 words
PROCESS FOR THE TEMPORARY PROTECTION OF AMINO GROUPS IN PEPTIDE SYNTHESES BY ACYLATING THE AMINO GROUP AND THEN ELIMINATING THE ACYL GROUP INTRODUCED, WHEREIN THE PROTECTIVE GROUP USED IS THE GROUP OF THE FORMULA I
Claim 2
Dependent Claim
35 words
PROCESS FOR THE TEMPORARY PROTECTION OF AMINO GROUPS IN PEPTIDE SYNTHESES BY ACYLATING THE AMINO GROUP AND THEN ELIMINATING THE ACYL GROUP INTRODUCED, WHEREIN THE PROTECTIVE GROUP USED IS THE GROUP OF THE FORMULA I
Claim 3
Dependent Claim
36 words
Process according to claim 1, wherein a group of the formula I is used in which R1 and R2 each represents a methyl or ethyl group and R3 has the same meaning as in claim 1.
Claim 4
Dependent Claim
32 words
Process according to claim 1, wherein a group of the formula I is used in which R3 represents a phenyl, tolyl or biphenylyl group and R1 and R2 stand for lower alkyl.
Claim 5
Dependent Claim
20 words
Process according to claim 1, wherein R1 stands for methyl or ethyl, and R2 and R3 each stands for phenyl.
Claim 6
Dependent Claim
21 words
Process according to claim 1, wherein the protective group of the formula I is the 2-phenyl-isopropyloxycarbonyl group or the 1,1-diphenylethyloxycarbonyl group.
Claim 7
Dependent Claim
17 words
Process according to claim 1, wherein the protective group of the formula I is the 2-para-tolylisopropyloxycarbonyl group.
Claim 8
Dependent Claim
17 words
Process according to claim 1, wherein the protective group of the formula I is the 2-(para-biphenylyl)-isopropyloxycarbonyl group.
Claim 9
Dependent Claim
28 words
Process according to claim 1, wherein the group of the formula I is used as a selectively eliminable Alpha -amino group in addition to acid-labile side-chain protective groups.
Claim 10
Dependent Claim
61 words
Process according to claim 1, wherein in the synthesis of peptides which in the side-chain contAin amino, hydroxy or carboxyl groups, the amino groups are protected by the tertiary butyloxycarbonyl group, the hydroxy group by the tert. butyl ether group and the carboxyl group by the tertiary butylester group and the Alpha -amino group by the group of the formula I.
Claim 11
Dependent Claim
37 words
Process according to claim 1, wherein, in the synthesis of peptides, containing mercapto groups in the side-chain, these groups are protected by the trityl group and the Alpha -amino group by the group of the formula I.
Claim 12
Dependent Claim
24 words
Process according to claim 1, wherein the group of the formula I is used in the synthesis of peptides by the solid phase synthesis.
Claim 13
Dependent Claim
31 words
Process according to claim 1, wherein the group of the formula I is introduced by means of its azide into Alpha -amino acids or into peptides consisting of Alpha -amino acids.
Claim 14
Dependent Claim
32 words
Process according to claim 1, wherein the group of the formula I is introduced by means of its phenyl ester into Alpha -amino acids or into peptides consisting of Alpha -amino acids.
Claim 15
Dependent Claim
19 words
N -Acyl- Alpha -aminoacids and derivatives thereof in which the acyl radical is a group of the formula I
Claim 16
Dependent Claim
19 words
N -Acyl- Alpha -aminoacids and derivatives thereof in which the acyl radical is a group of the formula I
Claim 17
Dependent Claim
42 words
N -Acyl- Alpha -aminoacids and derivatives thereof in which the acyl radical is a group of the formula I as claimed in claim 14 in which R1 and R2 each represents methyl or ethyl and R3 stands for phenyl, tolyl or biphenylyl.
Claim 18
Dependent Claim
39 words
N -Acyl- Alpha -aminoacids and derivatives thereof, in which the acyl radical is a group of the formula I as calimed in claim 14 in which R1 and R2 each represents methyl and R3 stands for a phenyl group.
Claim 19
Dependent Claim
37 words
N -Acyl- Alpha -aminoacids and derivatives thereof, in which the acyl radical is a group of the formula I as claimed in claim 14 in which R1 and R2 each represents methyl and R3 stands for para-biphenylyl.
Claim 20
Dependent Claim
39 words
N -Acyl- Alpha -aminoacids and derivatives thereof in which the acyl radical is a group of the formula I as claimed in claim 14 in which R1 and R2 each represents a methyl group, and R3 stands for para-tolyl.
References Cited (Backward Citations)
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1978-03-31 | 1978-09-30 | 1979-04-01 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1982-03-31 | 1982-09-30 | 1983-04-01 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1986-03-31 | 1986-09-30 | 1987-04-01 | $7700.00 | Window Closed / Lapsed |