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JPS59141583A Thiopyranopyrimidine derivative and its acid addition salt 失效
标题翻译：三硝基吡啶衍生物及其酸添加盐
公开(公告)号：JPS59141583A
公开(公告)日：1984-08-14
申请号：JP1509783
申请日：1983-02-01
申请人： Maruko Seiyaku Kk
发明人： OONO SACHIO , MIZUKOSHI SEISHI , KOMATSU OSAMU , YAMAMOTO HAJIME , KUNOU YASUO
IPC分类号： C07D495/04 , A61K31/505 , A61P3/08 , A61P3/10
摘要： NEW MATERIAL:The thiopyranopyrimidine derivative of formula I (R
1 is amino, hydroxyethylamino, piperazino, etc.; R
2 is amino, dimethylamino, morpholino, etc.).
EXAMPLE: 2-Amino-4-piperazino-7,8-dihydro-6H-thiopyrano[ 3,2-d ]-pyrimidine dimaleate.
USE: Remedy for diabetes.
PREPARATION: The compound of formula I wherein R
2 is NH
2 can be prepared by reacting 2-amino-4-chloro-7,8-dihydro-6H-thiopyrano[3,2-d]-pyrimidine of formula II (novel substance) with excessive amount of corresponding amine (e.g. ammonia, methylamine, etc.) in the absence or presence of a solvent such as dichloromethane at 0W100°C for 0.5W10hr. The starting compound of formula IIcan be obtained by reacting the compound of formula III with guanidine carbonate in the presence of a base, and reacting the resultant novel compound of formula IV with phosphorus oxychloride in the presence of N,N-dimethylaniline, etc.
COPYRIGHT: (C)1984,JPO&Japio
摘要翻译：新材料：式I的噻喃并嘧啶衍生物（R 1是氨基，羟乙基氨基，哌嗪基等; R 2是氨基，二甲基氨基，吗啉代等）。实施例：2-氨基-4-哌嗪基-7,8-二氢-6H-噻喃并[3,2-d] - 嘧啶二马来酸盐。用途：糖尿病补救。制备：其中R 2是NH 2的式I化合物可以通过使式II的2-氨基-4-氯-7,8-二氢-6H-噻喃并[3,2-d] - 嘧啶（新颖的物质）与过量的相应的胺（如氨，甲胺等）在0-100℃的溶剂（如二氯甲烷）存在或不存在下反应0.5-10小时。式II的起始化合物可以通过在碱的存在下使式III化合物与碳酸胍反应而得到，并在N，N-二甲基苯胺等的存在下，使得到的式Ⅳ的新化合物与磷酰氯反应。

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