Crystal modification of 2,4-diamino-6-hydroxymethylpteridine hyd

Details Crystal modification of 2,4-diamino-6-hydroxymethylpteridine hyd Crystal modification of 2,4-diamino-6-hydroxymethylpteridine hyd

1997-11-19

1999-06-08

Daus, Donald G.

Organic compounds -- part of the class 532-570 series

Organic compounds

Plural nitrogens bonded directly to the pteridine ring system

C02D42808

Patent

active

059105887

ABSTRACT:
A novel crystal modification of the compound 2,4-diamino-6-hydroxymethylpteridine hydrobromide and a process for its preparation and its use for preparing methotrexate. The novel crystal modification of 2,4-diamino-6-hydroxymethylpteridine hydrobromide is distinguished in particular by the fact that only one equivalent of the brominating agent triphenylphosphine dibromide is needed for brominating the 6-hydroxymethyl group. No reaction with the amino groups in the 2 and 4 positions takes place. This facilitates the reaction to give 2,4-diamino-6-pteridinyl derivatives such as methotrexate.

REFERENCES:
patent: 4077957 (1978-03-01), Piper et al.
patent: 4079056 (1978-03-01), Piper et al.
patent: 4080325 (1978-03-01), Ellard
patent: 4224446 (1980-09-01), Catalucci
patent: 4306064 (1981-12-01), Ellard

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