PYRIMIDINE COMPOUNDS, METHODS FOR THEIR PREPARING (VARIANTS), INTERMEDIATE SUBSTANCES (VARIANTS) AND METHODS FOR THEIR PREPARING (VARIANTS), METHOD FOR PREPARING TRIAZOLOPYRIMIDINE COMPOUNDS Russian patent published in 2007 - IPC C07D487/04 C07D405/12 C07D239/47 C07D317/44 C07D239/00 C07D317/00 C07D249/00 

Abstract RU 2295526 C2

FIELD: organic chemistry, chemical technology, medicine.

SUBSTANCE: invention relates to a method for improved synthesis of pharmacologically active compound of the formula (A): Method involves the following steps: (a) interaction of compound of the formula (I): with alkaline metal nitrite in the presence of suitable acid to yield compound of the formula (VII): (b) coupling compound of the formula (VII) with compound of the formula (VI): to yield compound of the formula (V): and (c) removal of protection from compound of the formula (V) to yield compound of the formula (A). Compound of the formula (A) possesses property of antagonist of R2T receptors, high metabolic stability and bioavailability. Also, invention relates to a novel intermediate substance of the formula (I) and methods for its synthesis, and to novel intermediate substances used in its synthesis.

EFFECT: improved method of synthesis, valuable medicinal properties of compounds.

12 cl, 4 ex

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RU 2 295 526 C2

Authors

Larsson Ul'F

Magnusson Mattias

Musil' Tibor

Pal'Mgren Andreas

Dates

2007-03-20Published

2001-05-31Filed