Process for preparing substituted pyrimidinones

Details Process for preparing substituted pyrimidinones Process for preparing substituted pyrimidinones

1983-07-27

1986-02-11

Daus, Donald G.

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

Organic compounds

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

544321, 546276, 548134, 548138, 548190, 548214, 549472, 549 75, C07D23902

Patent

active

045699968

ABSTRACT:
This invention provides a process for the preparation of pyrimidinone compounds with a group R.sup.2 CH(OH)-- at the 5-position thereof, wherein R.sup.2 is an optionally substituted acid-stable 5- or 6-membered nitrogen-containing heteroaryl group. The pyrimidinone ring is further substituted by a side-chain of a H.sub.1 -antagonist or H.sub.2 -antagonist or a precursor thereof.
The compounds are convertible to 5-heteroaryl methyl compounds which are either useful H.sub.1 - or H.sub.2 -antagonists or precursors thereof.

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Derwent Abstract 38240C(WP8000966).
Perrin, Dissociation Constants of Organic Bases in Aqueous Solution, (1965), pp. 213, 222.
Peter Sykes, A Guidebook to Mechanism in Organic Chemistry, (1961), p. 154.
Yoneda et al., Heterocycles, 12:691-694, (1979).

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