Di Braccio M, Roma G, Mazzei M, Balbi A, Testa R
Farmaco Sci. 1986 Mar;41(3):183-95.
Reaction of 2-aminothiazole with the N,N-dialkyl or (N-alkyl, N-phenyl) ethoxycarbonylacetamide/POCl3 reactant (I), in refluxing 1,2-dichloroethane, yielded the corresponding N,N-disubstituted 5-amino-7H-thiazolo[3,2-a]pyrimidin-7-ones (VII) along with lower quantities of isomeric N,N-disubstituted 7-amino-5H-thiazolo[3,2-a]pyrimidin-5-ones (VIII). Structures attributed to isomeric compounds (VII) and (VIII) were supported both by spectroscopic and chemical evidences. Some compounds (VII) were submitted to pharmacological investigation and results are described: only (N-alkyl, N-phenyl)derivatives (VII f,g) showed a significant, even if mild, activity as peripheral analgesics.
2-氨基噻唑与N,N-二烷基或（N-烷基，N-苯基）乙氧羰基乙酰胺/三氯氧磷反应物（I）在回流的1,2-二氯乙烷中反应，生成相应的N,N-二取代的5-氨基-7H-噻唑并[3,2-a]嘧啶-7-酮（VII）以及少量的异构体N,N-二取代的7-氨基-5H-噻唑并[3,2-a]嘧啶-5-酮（VIII）。通过光谱和化学证据支持了赋予异构体化合物（VII）和（VIII）的结构。一些化合物（VII）进行了药理研究，并描述了结果：只有（N-烷基，N-苯基）衍生物（VII f，g）表现出显著的，即使是温和的外周镇痛药活性。
