兰州大学学报(自然科学版)
蘭州大學學報(自然科學版)
란주대학학보(자연과학판)
JOURNAL OF LANZHOU UNIVERSITY(NATURAL SCIENCES)
2014年
6期
902-906
,共5页
李春新%陈立福%霍利春%刘生丽
李春新%陳立福%霍利春%劉生麗
리춘신%진립복%곽리춘%류생려
哌啶二酮%吲哚%盐酸阿洛司琼%合成%高产率
哌啶二酮%吲哚%鹽痠阿洛司瓊%閤成%高產率
고정이동%신타%염산아락사경%합성%고산솔
piperidinedione%indole%alosetron hydrochloride%synthesis%high yield
探索了以丙二酸单乙酯、3-氨基丙酸乙酯盐酸盐为原料合成2,4-哌啶二酮,再与N-甲基-2-苯肼反应生成目标分子2,3,4,5-四氢-5-甲基-1H-吡啶并[4,3-b]吲哚-1-酮和盐酸阿洛司琼的合成方法,总收率为30.2%.此方法反应速率快、产率高、适用于大规模生产.
探索瞭以丙二痠單乙酯、3-氨基丙痠乙酯鹽痠鹽為原料閤成2,4-哌啶二酮,再與N-甲基-2-苯肼反應生成目標分子2,3,4,5-四氫-5-甲基-1H-吡啶併[4,3-b]吲哚-1-酮和鹽痠阿洛司瓊的閤成方法,總收率為30.2%.此方法反應速率快、產率高、適用于大規模生產.
탐색료이병이산단을지、3-안기병산을지염산염위원료합성2,4-고정이동,재여N-갑기-2-분정반응생성목표분자2,3,4,5-사경-5-갑기-1H-필정병[4,3-b]신타-1-동화염산아락사경적합성방법,총수솔위30.2%.차방법반응속솔쾌、산솔고、괄용우대규모생산.
The synthesis method was used to obtain 2, 3, 4, 5-tetrahydro-5-methyl-1H-pyrido[4, 3-b]indol-1-one and alosetron hydrochloride from N-methyl-2-phenylhydrazine and 2, 4-piperidine-dione was synthesized with malonate and 3-amino-propionic acid ethyl ester hydrochloride. The overall yield of the compound was 30.2%The methods had a rapid reaction rate, high yield and were applicable in industrial production.