Document Type and Number:
Japanese Patent JPS6124394
Kind Code:
B2
Abstract:
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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Inventors:
JEEMUSU AARU PAIPAA
JON EI MONTOGOMERII
JON EI MONTOGOMERII
Application Number:
JP21536082A
Publication Date:
June 10, 1986
Filing Date:
December 08, 1982
Export Citation:
Assignee:
SAZAN RISAACHI INST
International Classes:
C07D475/08