上海应用技术学院学报:自然科学版
上海應用技術學院學報:自然科學版
상해응용기술학원학보:자연과학판
Journal of Shanghai Institute of Technology: Natural Science
2012年
1期
9-12
,共4页
陶晓虎%崔梦如%刘烽%欧文华%潘仙华
陶曉虎%崔夢如%劉烽%歐文華%潘仙華
도효호%최몽여%류봉%구문화%반선화
(R)-1-苄基-3-氨基吡咯烷%D-天冬氨酸%Dutogliptin%合成
(R)-1-芐基-3-氨基吡咯烷%D-天鼕氨痠%Dutogliptin%閤成
(R)-1-변기-3-안기필각완%D-천동안산%Dutogliptin%합성
(R)-l-benzylpyrrolidin-3-amine%D-aspartate%Dutogliptin%synthesis
(R)-1-苄基-3-氨基吡咯烷是合成抗糖尿病新药Dutogliptin的关键中间体。现以D-天冬氨酸为原料,通过氨基保护、内酸酐化、内酰胺化、脱保护和还原等五步反应,合成得到1-苄基-3-氨基吡咯烷,总产率为67.5%。该法具有原料便宜易得、操作简单、产物易于分离提纯等优点。
(R)-1-芐基-3-氨基吡咯烷是閤成抗糖尿病新藥Dutogliptin的關鍵中間體。現以D-天鼕氨痠為原料,通過氨基保護、內痠酐化、內酰胺化、脫保護和還原等五步反應,閤成得到1-芐基-3-氨基吡咯烷,總產率為67.5%。該法具有原料便宜易得、操作簡單、產物易于分離提純等優點。
(R)-1-변기-3-안기필각완시합성항당뇨병신약Dutogliptin적관건중간체。현이D-천동안산위원료,통과안기보호、내산항화、내선알화、탈보호화환원등오보반응,합성득도1-변기-3-안기필각완,총산솔위67.5%。해법구유원료편의역득、조작간단、산물역우분리제순등우점。
R)-l-benzylpyrrolidin-3-amine is the key intermediate of antidiabetic drug Dutogliptin. Starting from D-aspartate, the target compound can be obtained through five steps such as amino protection, anhydridation, amidation, removal of benzyl, and reduction. The total yield is about 67.5 %. Compared with other methods, this process was advantageous in synthesis in large scale and application due to the cheap and available materials and the easily separated and purified product.