药学研究
藥學研究
약학연구
JOURNAL OF PHARMACEUTICAL RESEARCH
2015年
1期
55-56
,共2页
苯甲酸阿格列汀%合成%改进
苯甲痠阿格列汀%閤成%改進
분갑산아격렬정%합성%개진
Alogliptin benzoate%Synthesis%Improvement
目的：改进苯甲酸阿格列汀的合成工艺。方法以6—氯尿嘧啶为起始原料，先与碘甲烷反应合成3—甲基—6—氯尿嘧啶，继而在无机碱的参与下与2—溴甲基苄腈反应得2—（6—氯—3甲基—2，4—二氯代—3，4—二氢—2H—嘧啶—1—基甲基）—苄腈，然后再在无机碱的存在下与（ R）—3—氨基哌啶二盐酸发生取代反应，最后与苯甲酸成盐得苯甲酸阿格列汀。结果合成得到苯甲酸阿格列汀，总收率达到57.09%，纯度为99.6%。结论该工艺经过改进，降低了毒害，成本降低，经济环保，适合工业化生产。
目的：改進苯甲痠阿格列汀的閤成工藝。方法以6—氯尿嘧啶為起始原料，先與碘甲烷反應閤成3—甲基—6—氯尿嘧啶，繼而在無機堿的參與下與2—溴甲基芐腈反應得2—（6—氯—3甲基—2，4—二氯代—3，4—二氫—2H—嘧啶—1—基甲基）—芐腈，然後再在無機堿的存在下與（ R）—3—氨基哌啶二鹽痠髮生取代反應，最後與苯甲痠成鹽得苯甲痠阿格列汀。結果閤成得到苯甲痠阿格列汀，總收率達到57.09%，純度為99.6%。結論該工藝經過改進，降低瞭毒害，成本降低，經濟環保，適閤工業化生產。
목적：개진분갑산아격렬정적합성공예。방법이6—록뇨밀정위기시원료，선여전갑완반응합성3—갑기—6—록뇨밀정，계이재무궤감적삼여하여2—추갑기변정반응득2—（6—록—3갑기—2，4—이록대—3，4—이경—2H—밀정—1—기갑기）—변정，연후재재무궤감적존재하여（ R）—3—안기고정이염산발생취대반응，최후여분갑산성염득분갑산아격렬정。결과합성득도분갑산아격렬정，총수솔체도57.09%，순도위99.6%。결론해공예경과개진，강저료독해，성본강저，경제배보，괄합공업화생산。
Pbjective To improve synthetic process of alogliptin benzoate. Methods Alogliptin benzoate was synthe-sized from 6—chlorine uracil and iodomethane to give 3 —methyl—6 —chlorine uracil,then in the presence of inorganic base with 2—bromine methyl benzonitrile reaction to 2—(6—methyl chloride—3—2,4—dichloro generation—3,4—di-hydro—2 h—pyrimidine—1—methyl)—benzonitrile,which was subjected to displacement with( R)—3—aminopiperidine in the presence of inorganic base. And then salified with benzoic acid to obtain alogliptin benzoate. ResuIts Alogliptin ben-zoate was synthesized. The overall yield was 57. 09%,and its purity was 99. 6%. ConcIusion The improvement reduced toxic,and was economic and environmental. It was suitable for industrial production.
