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US4701526A
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Process for preparing 9-(2-hydroxyethoxymethyl)-guanine, and intermediates useful in said process
Assignee: KRKA dd
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Filing: 1985-12-11
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Granted: 1987-10-20
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Expires: 2005-12-11
Abstract
Abstract There is disclosed a process for preparing 9-(2-hydroxyethoxymethyl)-guanine (acyclovir) of the formula IV ##STR1## wherein a novel compound of the formula I ##STR2## wherein R and R' may be the same or different and represent hydrogen, (C 1 -C 8 )acyl or benzyl and R 1 represents (C 1 -C 8 )acyl, is hydrolyzed under mild basic conditions. Also disclosed is the novel compound of the formula I, a process for the preparation thereof by condensing a novel compound of the formula II ##STR3## with a compound A--CH 2 --O--CH 2 CH 2 --OR' (A is a leaving group, Q is hydrogen or a leaving group), the novel compound of the formula II and a process for the preparation thereof by means of condensing glyoxal hydrate and a compound of the formula V ##STR4##
Inventors
- 👤 Joze Kobe
- 👤 Joze Gnidovec
- 👤 Pavle Zupet
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-30 17:04
CPC Classifications
C; C07; C07D; C07D473/00; C07D487/00; C07D487/12; C07D487/14
Claims Analysis
Total Claims: 17
Claim 1
Independent Claim
53 words
Process for preparing 9-(2-hydroxyethoxymethyl)-guanine of the formula ##STR11## characterized in that a compound of the formula I ##STR12## wherein R and R' may be the same or different and represent hydrogen, (C 1 -C 8 )acyl or benzyl and R 1 represents (C 1 -C 8 )acyl is hydrolyzed under mild basic conditions.
Claim 2
Dependent Claim
53 words
Process for preparing 9-(2-hydroxyethoxymethyl)-guanine of the formula ##STR11## characterized in that a compound of the formula I ##STR12## wherein R and R' may be the same or different and represent hydrogen, (C 1 -C 8 )acyl or benzyl and R 1 represents (C 1 -C 8 )acyl is hydrolyzed under mild basic conditions.
Claim 3
Dependent Claim
36 words
A compound of the formula I ##STR13## wherein R and R' may be the same or different and represent hydrogen, (C 1 -C 8 )acyl or benzyl and R 1 represents (C 1 -C 8 )acyl.
Claim 4
Dependent Claim
36 words
A compound of the formula I ##STR13## wherein R and R' may be the same or different and represent hydrogen, (C 1 -C 8 )acyl or benzyl and R 1 represents (C 1 -C 8 )acyl.
Claim 5
Dependent Claim
36 words
A compound of the formula II ##STR14## wherein R represents hydrogen, (C 1 -C 8 )acyl or benzyl, Q represents a hydrogen atom or a leaving group, and R 1 represents (C 1 -C 8 )acyl.
Claim 6
Dependent Claim
36 words
A compound of the formula II ##STR14## wherein R represents hydrogen, (C 1 -C 8 )acyl or benzyl, Q represents a hydrogen atom or a leaving group, and R 1 represents (C 1 -C 8 )acyl.
Claim 7
Dependent Claim
11 words
The compound of claim 2 wherein R is acetyl or isobutyryl.
Claim 8
Dependent Claim
10 words
The compound of claim 4 wherein R 1 is acetyl.
Claim 9
Dependent Claim
10 words
The compound of claim 2 wherein R 1 is acetyl.
Claim 10
Dependent Claim
11 words
The compound of claim 3 wherein R is acetyl or isobutyryl.
Claim 11
Dependent Claim
10 words
The compound of claim 7 wherein R 1 is acetyl.
Claim 12
Dependent Claim
10 words
The compound of claim 3 wherein R 1 is acetyl.
Claim 13
Dependent Claim
14 words
The compound of claim 2 wherein R is acetyl and R 1 is acetyl.
Claim 14
Dependent Claim
14 words
The compound of claim 3 wherein R is acetyl and R 1 is acetyl.
Claim 15
Dependent Claim
9 words
The compound of claim 3 wherein Q is acetyl.
Claim 16
Dependent Claim
17 words
The compound of claim 3 wherein R is acetyl, R 1 is acetyl, and Q is acetyl.
Claim 17
Dependent Claim
10 words
The compound of claim 10 wherein R 1 is acetyl.
References Cited (Backward Citations)
US4495190A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1990-10-19 | 1991-04-20 | 1991-10-20 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1994-10-19 | 1995-04-20 | 1995-10-20 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1998-10-19 | 1999-04-20 | 1999-10-20 | $7700.00 | Window Closed / Lapsed |