发明名称 |
A pteridine derivative and a process for the preparation of 10-deazaaminopterin and its derivatives from the pteridine derivative. |
摘要 |
There is disclosed an improved process for the preparation of 10-deazaaminopterin and related compounds. In accordance with this process, 6-(bromomethyl)-2,4-pteridinediamine hydrobromide is reacted with triphenyl-phosphine to form a phosphonium salt which is then treated with a base to yield the corresponding ylid (2,4-diamino-6-pteridinyl)methylenetriphenylphosphorane. This compound is reacted with an aromatic aldehyde such as diethyl 4-formylbenzoyl-L-glutamate to form an olefin which is then reduced catalytically to the tetrahydro derivative of the desired product. Oxidation of the tetrahydro derivative is accomplished with hydrogen peroxide.
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申请公布号 |
EP0006123(A1) |
申请公布日期 |
1980.01.09 |
申请号 |
EP19790101405 |
申请日期 |
1979.05.08 |
申请人 |
SOUTHERN RESEARCH INSTITUTE |
发明人 |
PIPER, JAMES R.;MONTGOMERY, JOHN A. |
分类号 |
C07D475/08;(IPC1-7):C07D475/08;C07F9/65 |
主分类号 |
C07D475/08 |
代理机构 |
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