87253-78-9Relevant articles and documents
A preparation method of the emetic (by machine translation)
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Paragraph 0028; 0033; 0038; 0044; 0049; 0051; 0054; 0058, (2019/04/17)
The invention relates to the field of organic synthetic technology, in particular to a emetic preparation method, comprises the following steps: S1, 3 - methoxy methyl acrylic acid methyl ester preparation; S2, synthesis of [...]; S3, is the synthesis of third zuo; S4, and aldehyde; S5, closed-loop. This invention adopts the single melamine as the synthetic starting material, greatly reducing the cost, dicyandiamide as to effectively solve the problem of lack of raw material sources; solved in the prior art long reaction time, the reaction condition is sensitive, harsh, side reaction are numerous and complex, the use of expensive or difficult to prepare sodium of other reagents, reactions caused low overall yield, the product quality is poor, so that the synthesis process technology of the route is more stable, good reproducibility, high yield, the product quality is good, content can be up to 99.5%, the yield can reach 85.6%, has higher economic benefits. (by machine translation)
Process for preparing triazolopyrimidine derivatives
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, (2008/06/13)
A process for preparing triazolopyrimidine derivatives of the formula (I): wherein R1represents a hydrogen or an alkyl radical of one to ten carbon atoms, or a cycloalkyl radical of three to six carbon atoms, or an alkenyl radical of up to four carbon atoms; R2represents a hydrogen, a halogen atom, a hydroxyalkyl or alkyl radical of one to ten carbon atoms; R3represents a hydrogen, a hydroxyalkyl or alkyl radical of one to four carbon atoms; by rapidly preparing diamino-1,2,4-triazole which is reacted with an aldehyde to form an imide which is reacted with an α,β-unsaturated acid derivative, the reaction product of which is hydrolyzed in the presence of an acid to produce the triazolopyrimidine derivatives of formula (I). The compounds of the formula (I) are capable of preventing bronchospasm.
Dialkyl bicyclic heterocycles with a bridgehead nitrogen as purine analogs possessing significant cardiac inotropic activity
Okabe,Bhooshan,Novinson,et al.
, p. 735 - 751 (2007/10/02)
A number of 5,7-dialkyl-s-triazolo[1,5-a]pyrimidines and 5,7-dialkylpyrazolo[1,5-a]pyrimidines and related heterocycles containing a bridgehead nitrogen have been prepared and studied as cardiovascular agents in the anesthetized dog. A number of these compounds have exhibited significant inotropic activity with little effct on heart rate. Especially active were 5,7-dialkyl-2-amino or 2-alkylthio-2-triazolo[1,5-a]pyrimidines. In contrast, highly polar purine analogs in these ring systems compounds such as 5,7-di-n-propyl-2-benzylthio-1,3,4-thiadiazolo[3,2-a]pyrimidine bromide 45 containing a charge on the bridgehead nitrogen, were inactive. The detailed structure activity relationship of the dialkyl derivatives of related ring systems are discussed. The presence of certain ring nitrogen atoms are vital to potent in vivo activity, presumably due to specific enzyme binding at these sites. Several of the compounds studied, showed oral activity and are excellent candidates for further evaluation in man.