摘要
本文摸索了＂顽固＂氨基酸-天冬酰胺与氯甲基聚苯乙烯生成苄酯的几种方法。首次发现二环已胺（ＤＣＨＡ），Ｎ-苄基三甲基氢氧化铵（ＴｒｉｔｏｎＢ）及Ｃｓ２ＣＯ３／ＫＩ等催化条件下获得苄酯产物的收率（５４．８％，６８．１％及７６．５％），均明显优于文献报道值（＜３３．５％）。
Being the characteristic side-chain amide group,asparagine and glutamine possess some special physical and chemical properties. In the present study ,we tried to find out the optimum condition for the preparation of Boc-OCH2-polystyrene(1).Couple of bases such as Cs2CO3,KOH,DEA and TEA were not ready to induce the esterification of Boc-Asn and BocGln with chloromethyl resin in our hands。 By the aiding of DCHA(dicyclohexylamine)or Triton B(N-benzyltrimethyl ammonium hydroxide),product(1)could be detected with the yield of 54.8%and 68.1%respectively。potassium halides were explored as the catalyst assisting Cs2CO3 in producing (1). Reasonable yields ,64.4%(from KF / Cs2CO3), 29.1%(from KBr/Cs2CO3)and 76.5%(from KI/Cs2CO3),were found also.
出处
《中国药物化学杂志》
CAS
CSCD
1994年第3期209-211,共3页
Chinese Journal of Medicinal Chemistry
基金
国家自然科学基金
关键词
天冬酰胺
苄酯化
聚苯乙烯
合成
药物化学
Asparagine
Benzyl-esterification
Solid-phase peptide synthesis
