首页> 外国专利> 2- 2- (substituted amino) benzylthio -5,6,7,8-tetrahydropyrido 3,4-d pyrimidin -4 (3H) - one derivatives

2- 2- (substituted amino) benzylthio -5,6,7,8-tetrahydropyrido 3,4-d pyrimidin -4 (3H) - one derivatives

机译:2- [2-(取代的氨基)苄硫基] -5,6,7,8-四氢吡啶并[3,4-d]嘧啶-4(3H)-一种衍生物

摘要

PURPOSE: To obtain a compound excellent in gastric inhibitory effect and gastrointestinal mucosa protecting effect on gastric ulcer and duodenal ulcer model and useful as an anti-peptic ulcer agent excellent in safety. ;CONSTITUTION: A compound (salt) of formula I (R1 and R2 are each H or a lower alkyl; R3 and R4 are each a lower alkyl), e.g. 2-[2-(N,N-diethylamino) benzylthio]-5,6,7,8-tetrahydropyrido[3,4-α]pyrimidin-4(3H)one. This compound is obtained, e.g. by reacting a compound of formula II with a compound of formula III in the presence of a base such as sodium hydroxide in a solvent such as methanol at -10°C to the solvent reflux temperature for 10min to 24hr to synthesize a compound of formula IV through an S-benzylation reaction and then reacting a compound of formula R1X (X is Cl, Br, I, methanesulfonyloxy, etc.) therewith in the presence of a base in a solvent such as methanol at -10°C to the solvent reflux temperature for 1 to 48hr.;COPYRIGHT: (C)1995,JPO
机译:目的:获得对胃溃疡和十二指肠溃疡模型具有优异的胃抑制作用和胃肠道粘膜保护作用的化合物,并可用作安全性优异的抗消化性溃疡剂。 ;组成:式Ⅰ的化合物(盐)(R 1 和R 2 分别为H或低级烷基; R 3 和R 4 均为低级烷基),例如2- [2-(N,N-二乙氨基)苄硫基] -5,6,7,8-四氢吡啶并[3,4-α]嘧啶-4(3H)one。获得该化合物,例如。在碱例如氢氧化钠存在下,在溶剂例如甲醇中,于-10℃使式II化合物与式III化合物反应至溶剂回流温度10分钟至24小时,以合成式IV化合物通过S-苄基化反应,然后使式R 1 X的化合物(X为Cl,Br,I,甲磺酰氧基等)在碱的存在下在溶剂如甲醇中与之反应在-10°C到溶剂回流温度1到48小时;版权:(C)1995,JPO

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