- Synthetic method for high-purity 6-furfurylaminopurine
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The invention discloses a synthetic method for high-purity 6-furfurylaminopurine. According to the synthetic method, in the existence of 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU), furfuryl amine and 6-chloropurine are subjected to nucleophilic substitution reaction under reflux condition of hexamethyldisilazane so as to obtain a crude product of 6-furfurylaminopurine, and recrystallizing is carriedout so as to obtain 6-furfurylaminopurine, the HPLC purity is 99.5% or above, and the any individual impurity content is less than 0. 1wt%. The synthetic method has the advantages of being simple inprocess, high in yield and free of wastewater discharge.
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Paragraph 0012-0014
(2018/12/14)
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- The scope and mechanism of phosphonium-mediated SNAr reactions in heterocyclic amides and ureas
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(Chemical Equation Presented) An efficient "one-step" synthesis of cyclic amidines and guanidines has been developed. Treatment of cyclic amides and ureas with benzotriazol-l-yloxytris(dimethylamino)phosphonium hexafluorophosphate (BOP), base, and nitrogen nucleophiles leads to the formation of the corresponding cyclic amidines and guanidines, typically in good to excellent yields. This method has also been used to prepare heteroaryl ethers and thioethers using phenol and thiophenol nucleophiles. Time course NMR and HPLC-MS studies have facilitated explicit characterization of the proposed intermediates (the phosphonium salt and HOBt adduct); the data reveal a stepwise reaction pathway.
- Wan, Zhao-Kui,Wacharasindhu, Sumrit,Levins, Christopher G.,Lin, Melissa,Tabei, Keiko,Mansour, Tarek S.
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p. 10194 - 10210
(2008/04/12)
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- An efficient direct amination of cyclic amides and cyclic ureas
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An efficient one-step amination of cyclic amides and ureas has been developed. Treatment of cyclic amides and cyclic ureas with BOP in the presence of DBU in various solvents led to the formation of cyclic amidines and cyclic guanidines in good to excellent yields. Concise syntheses of biologically intriguing kinetin and potent kinase inhibitor olomoucin were thus achieved in just one and two steps, respectively.
- Wan, Zhao-Kui,Wacharasindhu, Sumrit,Binnun, Eva,Mansour, Tarek
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p. 2425 - 2428
(2007/10/03)
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