US3714140A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Peptide synthesis
Assignee: ER Squibb and Sons LLC
•
Filing: 1971-03-16
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Granted: 1973-01-30
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Expires: 1991-03-16
Abstract
Abstract An improved solid phase process for peptide synthesis wherein all steps of the synthesis are carried out in a solvent which produces a highly swollen state in the resin and wherein the coupling agent employed is one which forms by-products which are soluble in the solvent.
Inventors
- 👤 F Sipos
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-08 03:33
CPC Classifications
C; C07; C07K; C07K1/00; C07K1/10; C07K1/04
Claims Analysis
Total Claims: 9
Claim 1
Independent Claim
90 words
In a process for the preparation of a peptide wherein an N-protected amino acid or peptide is coupled by means of a coupling agent to the unprotected N-terminal amino group of an amino acid or peptide which amino acid or peptide is coupled at its C-terminal group to an insoluble resin, the improvement comprising carrying out the coupling and cleavage steps of the synthesis in a solvent which produces a highly swollen state in the resin, and employing a coupling agent which forms by-products that are soluble in the solvent.
Claim 2
Dependent Claim
90 words
In a process for the preparation of a peptide wherein an N-protected amino acid or peptide is coupled by means of a coupling agent to the unprotected N-terminal amino group of an amino acid or peptide which amino acid or peptide is coupled at its C-terminal group to an insoluble resin, the improvement comprising carrying out the coupling and cleavage steps of the synthesis in a solvent which produces a highly swollen state in the resin, and employing a coupling agent which forms by-products that are soluble in the solvent.
Claim 3
Dependent Claim
12 words
A process according to claim 1 wherein the coupling agent is N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline.
Claim 4
Dependent Claim
19 words
A process according to claim 1 wherein the solvent is DMF or a halogenated alkane, or a mixture thereof.
Claim 5
Dependent Claim
11 words
A process according to claim 3 wherein the solvent is dichloromethane.
Claim 6
Dependent Claim
29 words
A process according to claim 1 wherein the protected N-terminal amino group is deprotected and another amino acid or peptide is coupled to the resulting deprotected N-terminal amino group.
Claim 7
Dependent Claim
23 words
A process according to claim 5 wherein the deprotecting and coupling steps are repeated as often as required to form the desired peptide.
Claim 8
Dependent Claim
11 words
A process according to claim 2 wherein the solvent is dichloromethane.
Claim 9
Dependent Claim
17 words
A process according to claim 5 wherein the coupling agent is N-ethoxycarbonyl-2-ethoxy-1,2-dihydroquinoline and the solvent is dichloromethane.
References Cited (Backward Citations)
GB1218459A
Cited
US3563958A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1976-01-30 | 1976-07-31 | 1977-01-30 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1980-01-30 | 1980-07-31 | 1981-01-30 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1984-01-30 | 1984-07-31 | 1985-01-30 | $7700.00 | Window Closed / Lapsed |