Synthesis of 2-substitudephenoxy-5-benzyloxypyrimidines compounds
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摘要: 目的 探索2-取代苯氧基-5-苯甲氧基嘧啶、2-取代苯氧基-5-羟基嘧啶类化合物的制备方法。 方法 以2-氯-5-羟基嘧啶为起始原料,经溴苄羟基保护、威廉森醚合成法、脱苄基保护等多步反应制得目标化合物。 结果 采用该合成路线制得13个未见文献报道的取代苯氧基嘧啶类化合物。 结论 本研究提出了一条操作简便、条件温和的全新苯氧基嘧啶类化合物合成方法。
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关键词:
- 2-取代苯氧基-5-苯甲氧基嘧啶 /
- 2-取代苯氧基-5-羟基嘧啶 /
- 合成
Abstract: Objective To prepare 2-substitudephenoxy-5-benzyloxypyrimidines and 2-substitudephenoxy-5-hydroxypyrimidines which had not been reported. Methods The target compounds were prepared from 2-chlorine-5-hydroxypyrimidine through hydroxy protection, Williamsom reaction and reduction of benzyl group. Results The synthetic process provided a simple, easy diposal procedure and high overall yield. Fourteen new phenoxy pyrimidines compounds were prepared. Conclusions It was a new synthetic method which was easy to operate with moderate reaction conditions. -
[1] Zoller G,Schmoll D,Mueller M,et al. Heterocyclic compounds, processes for their preparation, medicaments comprising these compounds, and the use thereof[P].WO,2010003624,2010-01-14. [2] Okada H,Koyanagi T,Yamada N,et al.Synthesis and anxiolytic activity of N-substituted cyclic imides (1R*,2S*3R*,4S*)-N-[4-[4-(2-Pyrimidinyl)-1-piperazinyl]butyl]--2,3-bicyclo[2.2.1] heptanedicarboximide(Tandospirone) and related compounds[J].Chem Pharm Bull,1991,39:1308. [3] Susheel JN,Mukund J,Johan B,et al.A simple Cu-catalyzed coupling approach to substituted 3-Pyridinol and 5-Pyrimidinol antioxidants[J].J Org Chem, 2008,73(23):9326. [4] Chapman D,Gabos B,Munck RM,et al.Preparation of hydantoin derivatives for use as MMP inhibitors[P].WO,2008065393,2008-06-05. -
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