2,4-Diamino-pyrimidine derivatives and processes

Details 2,4-Diamino-pyrimidine derivatives and processes 2,4-Diamino-pyrimidine derivatives and processes

1975-06-26

1977-07-05

Daus, Donald G.

Chemistry of carbon compounds

Miscellaneous organic carbon compounds

C-metal

260465F, 424251, C07D23922

Patent

active

040339629

ABSTRACT:
The present invention relates to a new synthesis for the preparation of 5-(substituted benzyl)-2,4-diamino-pyrimidines, including new pyrimidine derivatives. More particularly, a new synthesis of ormetoprin, diaveridine and related compounds, including novel derivatives, is disclosed. The synthesis involves the condensation of a substituted benzene and an acrylonitrile derivative to directly give enol ether intermediates, which upon subsequent reaction by known techniques with guanidine, provides the desired 5-(substituted benzyl)-2,4-diamino-pyrimidines, including novel compounds. The pyrimidine end products are useful as potentiators of sulfonamides and as antibacterial agents.

REFERENCES:
patent: 2658897 (1953-11-01), Hitchings et al.
patent: 3341541 (1967-09-01), Hoffer
patent: 3496211 (1977-02-01), Dexter et al.
patent: 3852450 (1974-12-01), Silvestri et al.
patent: 3855265 (1974-12-01), Cresswell et al.
patent: 3956327 (1976-05-01), Cresswell et al.
patent: 3984460 (1976-10-01), Spivack

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