Method of preparing quinazolone derivatives

专利摘要:
Compounds of the formula <IMAGE> wherein A is -CH=CH-, -CH=N- or -S-, R1 is hydrogen, lower alkyl, lower alkoxy, amino, acetylamino, cyano, tetrazol-5-yl, -COR3 or a fused benzene ring, WHERE R3 is lower alkoxy, amino, hydroxyamino, tetrazol-5-yl-amino or, when R2 is other than hydrogen, also hydroxyl, and R2 is cyano, tetrazol-5-yl, -COR4 or, when R1 is cyano, tetrazol-5-yl or -COR3, also hydrogen, lower alkyl, lower alkoxy, amino, acetylamino or a fused benzene ring, WHERE R4 is lower alkoxy, amino, hydroxyl, hydroxyamino or tetrazol-5-yl-amino; NON-TOXIC, PHARMACOLOGICALLY ACCEPTABLE ACID ADDITION SALTS THEREOF; AND, WHEN R3 and/or R4 are hydroxyl, non-toxic, pharmacologically acceptable salts thereof formed with an inorganic or organic base. The compounds as well as their salts are useful primarily as antiallergics.
公开号:SU784776A3
申请号:SU782633660
申请日:1978-07-12
公开日:1980-11-30
发明作者:Шромм Курт；Ментруп Антон；Рент Эрнст-Отто；Фюгнер Армин
申请人:К.Х.Берингер Зон (Фирма)；
IPC主号:

专利说明:

The hydrolysis is also carried out with sodium hydroxide at or at the boiling point of the reaction mixture. Yield 1.2 g (41.1%).
Example 2. 11-Oxo-11-H-2-methylpyrido-2,1-L-quinazoline-8-carboxylic acid.
5 g of 8-cyano-11-oxo-11-H-2-methylpyrido-f2, 1-β-quinazoline is heated for 1 hour in a mixture of 10 ml of water, 10 ml of concentrated sulfuric acid, and 10 ml of glacial acetic acid . The precipitated crystals are sucked off, washed with water and acetonitrile. From the raw material, the final product is obtained in water with a calculated amount of sodium bicarbonate and acidification with acetic acid.
Found,%: C 66.23, H4.07, N 11.15.
“AHjoNaOj.
Calculated,%: C 66.14, H 3.94, N 11.02.
The output of 4.6 g (85%). Example 3. 13-OXO-13-H-benzo-Cd} -pyrido-quinazoline-10-carboxylic acid.
4 g of 13-oxo-13-H-benzod-pyrido-2,1-L-quinazoline-10-carboxamide in 80 ml of half-diluted hydrochloric acid are boiled for 5 hours. The precipitated crystals are washed with water and ra; Target yut. in diluted ammonia. The solution is extracted and, after filtration over active carbon, acidified with acetic acid. The resulting free acid is converted into hydrochloride, with concentrated hydrochloric acid, and yellow hydrochloride crystals are obtained.
Calculated,%: C 62.48, H 3.37, N 8.58, C I 10.87.
 CE
Found: C, 62.59; H, 3.48; N, 8.38; Cl, 10.23. 5 Yield 3.7 g (13%).

权利要求:
Claims (1)
[1]
Invention Formula
The method of obtaining derivatives chi10 nazolone of General formula (I)
ABOUT
BUT.
noos-4 an
where R is methyl, methoxy, or a condensed benzene ring, o t is l, and in that the compound of the general formula (Q)
where R denotes an ester group, amide or nitrile of carboxylic acid,
subjected to basic or acid hydrolysis.
Sources of information taken into account during the examination 1. Buhler K., Pearson D. Organic syntheses. M., Mir, 1973, Part 2, p. 223-229.

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法律状态:

优先权:

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申请号 | 申请日 | 专利标题

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DE2557425A|DE2557425C2|1975-12-19|1975-12-19|

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