US4115650A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Process for preparing 2,4-diamino-5-(substituted benzyl)-pyrimidines
Assignee: Hoffmann La Roche Inc
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Filing: 1976-11-17
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Granted: 1978-09-19
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Expires: 1996-11-17
Abstract
Abstract 2,4-Diaminopyrimidines bearing a substituted benzyl group in position-1 are prepared from the correspondingly substituted α-alkoxymethylcinnamonitrile by treatment of the latter with an alkali metal alkoxide in mono-methyl ether of ethylene glycol and subsequently reacting the resulting reaction mixture with guanidine.
Inventors
- 👤 Percy Manchand
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-08 14:54
CPC Classifications
C; C07; C07D; C07D239/00; C07D239/02; C07D239/24; C07D239/28; C07D239/46; C07D239/48; C07D239/49; C07C; C07C255/00
Claims Analysis
Total Claims: 3
Claim 1
Independent Claim
104 words
A process for the preparation of 2,4-diamino-pyrimidines of the formula ##STR5## wherein R 1 is hydrogen or lower alkyl; R 2 is hydrogen or lower alkoxy; R 3 is lower alkoxy or lower alkyl; R 4 is hydrogen or lower alkoxy; and R 2 and R 3 , when taken together, are methylenedioxy, which comprises the steps of treating the correspondingly substituted α-alkoxymethylcinnamonitrile with an alkali metal alkoxide in 2-methoxyethanol and an alkanol of the formula ROH, wherein R is lower alkyl, and treating the resulting reaction mixture with guanidine at a temperature in the range of from about 100° to about 140° C.
Claim 2
Dependent Claim
104 words
A process for the preparation of 2,4-diamino-pyrimidines of the formula ##STR5## wherein R 1 is hydrogen or lower alkyl; R 2 is hydrogen or lower alkoxy; R 3 is lower alkoxy or lower alkyl; R 4 is hydrogen or lower alkoxy; and R 2 and R 3 , when taken together, are methylenedioxy, which comprises the steps of treating the correspondingly substituted α-alkoxymethylcinnamonitrile with an alkali metal alkoxide in 2-methoxyethanol and an alkanol of the formula ROH, wherein R is lower alkyl, and treating the resulting reaction mixture with guanidine at a temperature in the range of from about 100° to about 140° C.
Claim 3
Dependent Claim
30 words
A process in accordance with claim 1, wherein the treatment of the substituted α-alkoxymethylcinnamonitrile with an alkali metal alkoxide is carried out at the reflux temperature of the reaction mixture.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1981-09-18 | 1982-03-20 | 1982-09-19 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1985-09-18 | 1986-03-20 | 1986-09-19 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1989-09-18 | 1990-03-20 | 1990-09-19 | $7700.00 | Window Closed / Lapsed |