Patent EP0075880A2 successfully refreshed from Google Patents.
EP0075880A2
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Pyrido (2,3-d) pyrimidines
Assignee: Southern Research Institute
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Filing: 1982-09-24
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Granted: —
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Expires: 2002-09-24
Abstract
Abstract There are disclosed novel intermediates useful in the preparation of pyrido[2,3-d] pyrimidines having the following structures: 0 wherein R is CH 3 , CH 3 CH 2 , CH 3 CH 2 CH 2 , CH 2 =CHCH 2 or CH CCH 2 ; and wherein R is CH 3 , CH 3 CH 2 , CH 3 CH 2 CH 2 , CH 2 =CHCH 2 or CH CCH 2 . These intermediates have the formulas: and wherein Y is CHO, CH 2 OH or CH 2 Br; and Z is CH 2 OH or CH 2 Br.
Inventors
- 👤 Carroll Glenn Temple, Jr.
- 👤 John Atterbury Montgomery
- 👤 Robert Daryl Elliott
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-02 19:03
CPC Classifications
C; C07; C07D; C07D471/00; C07D471/02; C07D471/04; C07F; C07F9/00; C07F9/02; C07F9/547; C07F9/6561
Claims Analysis
Total Claims: 18
Claim 1
Independent Claim
50 words
. Intermediates useful in the production of 5-deaza analogs of folic acid, N 10 -substituted folic acid, aminopterin, and N 10 -substituted aminopterin comprising compounds having the structures: and wherein Y is CHO, CH 2 OH or CH 2 Br; and Z is CH 2 OH or CH 2 Br.
Claim 2
Dependent Claim
50 words
. Intermediates useful in the production of 5-deaza analogs of folic acid, N 10 -substituted folic acid, aminopterin, and N 10 -substituted aminopterin comprising compounds having the structures: and wherein Y is CHO, CH 2 OH or CH 2 Br; and Z is CH 2 OH or CH 2 Br.
Claim 3
Dependent Claim
1 words
2,4-Diamino-6-(carboxaldehyde)pyrido-[2,3-d]pyrimidine.
Claim 4
Dependent Claim
1 words
2,4-Diamino-6-(carboxaldehyde)pyrido-[2,3-d]pyrimidine.
Claim 5
Dependent Claim
1 words
2,4-Diamino-6-(hydroxymethyl)pyrido[2,3-d]pyrimidine.
Claim 6
Dependent Claim
1 words
2,4-Diamino-6-(hydroxymethyl)pyrido[2,3-d]pyrimidine.
Claim 7
Dependent Claim
38 words
The 5-deaza analog of N 10 -substituted folic acid having the formula: wherein R is CH 3 , CH 3 CH 2 , CH 3 CH 2 CH 2 , CH 2 =CHCH 2 or CH≡CCH 2 .
Claim 8
Dependent Claim
38 words
The 5-deaza analog of N 10 -substituted folic acid having the formula: wherein R is CH 3 , CH 3 CH 2 , CH 3 CH 2 CH 2 , CH 2 =CHCH 2 or CH≡CCH 2 .
Claim 9
Dependent Claim
37 words
The 5-deaza analog of N 10 -substituted aminopterin having the formula: wherein R is CH 3 , CH 3 CH 2 , CH 3 CH 2 CH 2 , CH 2 =CHCH 2 or CH≡CCH 2 .
Claim 10
Dependent Claim
37 words
The 5-deaza analog of N 10 -substituted aminopterin having the formula: wherein R is CH 3 , CH 3 CH 2 , CH 3 CH 2 CH 2 , CH 2 =CHCH 2 or CH≡CCH 2 .
Claim 11
Dependent Claim
11 words
A compound as defined in claim 4 wherein R is methyl.
Claim 12
Dependent Claim
11 words
A compound as defined in claim 5 wherein R is methyl.
Claim 13
Dependent Claim
74 words
A process for preparing the dialkyl esters of 5-deaza analogs of folic acid, N 10- substituted folic acid, aminopterin or N 10 -substituted aminopterin which comprises reacting a compound as defined in claim 1 with a p-aminobenzoyl-L-glutamate having the formula: wherein R is CH 3 , CH 3 CH 2 , CH 3 CH 2 CH 2 , CH 2 = CHCH 2 or CH≡CCH 2 and R 1 is a lower alkyl group.
Claim 14
Dependent Claim
19 words
A process as defined in claim 8 wherein each R 1 is ethyl and R is hydrogen or methyl.
Claim 15
Dependent Claim
23 words
A process as defined in claim 8 wherein R is other than hydrogen and the groups Y and Z are CH 2 Br.
Claim 16
Dependent Claim
24 words
A method for preparing the compound defined in claim 7 which comprises methylating 5-deazaaminopterin by reaction with formaldehyde in the presence of sodium cyanoborohydride.
Claim 17
Dependent Claim
25 words
A method for preparing the compound defined in claim 6 which comprises methylating 5-deazafolic acid by reaction with formaldehyde in the presence of sodium cyanoborohydride.
Claim 18
Dependent Claim
24 words
A method for preparing the compound defined in claim 6 which comprises hydrolyzing the 4-amino group on 5-deazamethotrexate by treating 5-deazamethotrexate with a base.
References Cited (Backward Citations)
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