Process for preparing 2,4-dihaloquinazolines

Details Process for preparing 2,4-dihaloquinazolines Process for preparing 2,4-dihaloquinazolines

1977-06-20

1978-07-25

Rush, Raymond V.

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

Organic compounds

Nitrogen attached directly or indirectly to the purine ring...

560 29, 560 32, 544286, 544285, C07D23995

Patent

active

041028856

ABSTRACT:
A one-step process for the preparation of 2,4-dihaloquinazolines is disclosed beginning with methoxycarbonyl- or phenoxycarbonyl-derivatives of substituted phenylureas which are cyclized and concomitantly halogenated with a cyclizing-halogenating reagent such as N,N-dimethylaniline in phosphorus oxychloride. The 2,4-dihaloquinazolines of the instant process are particularly valuable as intermediates in the preparation of 4-amino-2-(4-substituted-piperazin-1-yl) quinazolines useful in the treatment of cardiovascular disorders such as hypertension.

REFERENCES:
patent: 3511836 (1970-05-01), Hess
patent: 3517005 (1970-06-01), Cronin et al.
patent: 3769286 (1973-10-01), Hess
patent: 3843652 (1974-10-01), Findeisen et al.
Curd et al., J. Chem. Soc., 1759 (1948).
Findeisen et al. (II), Synthesis, 599-605 (1972).
Budesinsky et al., Coll. Czech. Chem. Commun., 37, 2779 (1972).

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