南华大学学报:自然科学版
南華大學學報:自然科學版
남화대학학보:자연과학판
Journal of University of South China(Science and Technology)
2011年
4期
102-104
,共3页
夏岳韬%肖新荣%王英%贾小鹏%陈川
夏嶽韜%肖新榮%王英%賈小鵬%陳川
하악도%초신영%왕영%가소붕%진천
1-(2-氟苯基)-2-溴-1-丙酮%苯甘氨醇%吗啉醇盐酸盐%合成
1-(2-氟苯基)-2-溴-1-丙酮%苯甘氨醇%嗎啉醇鹽痠鹽%閤成
1-(2-불분기)-2-추-1-병동%분감안순%마람순염산염%합성
1-(2-difluorophenyl)-2-bromo-1-Acetone%Phenylglycinol%morpholinol hydrochloride%synthesis
以安非他酮在人体内的活性代谢物羟基安非他酮为先导化合物,利用1-(2-氟苯基)-2-溴-1-丙酮和苯甘氨醇在NMP溶剂中反应,经胺化、环合、酸化合成得到了吗啉环上5位含苯基的新型吗啉醇类化合物.总收率70.3%,新化合物结构经IR1、HNMR、MS确证.该化合物在国内外未见报道.整个合成路线具有反应时间短,条件温和、收率高等优点.
以安非他酮在人體內的活性代謝物羥基安非他酮為先導化閤物,利用1-(2-氟苯基)-2-溴-1-丙酮和苯甘氨醇在NMP溶劑中反應,經胺化、環閤、痠化閤成得到瞭嗎啉環上5位含苯基的新型嗎啉醇類化閤物.總收率70.3%,新化閤物結構經IR1、HNMR、MS確證.該化閤物在國內外未見報道.整箇閤成路線具有反應時間短,條件溫和、收率高等優點.
이안비타동재인체내적활성대사물간기안비타동위선도화합물,이용1-(2-불분기)-2-추-1-병동화분감안순재NMP용제중반응,경알화、배합、산화합성득도료마람배상5위함분기적신형마람순류화합물.총수솔70.3%,신화합물결구경IR1、HNMR、MS학증.해화합물재국내외미견보도.정개합성로선구유반응시간단,조건온화、수솔고등우점.
3-methyl-5-phenyl-(2-difluorophenyl)-2-morpholinol Hydrochloride was synthesized from 1-(2-difluorophenyl)-2-bromo-1-Acetone and Phenylglycinol in polar solvents NMP by amine,cyclization reaction,reduction and acidification.The yield amounted to 70.3%.The structures of the target compounds were confirmed by means of IR,1H NMR and MS spectra.This new compound has never been reported at home and abroad.The synthesis method in the article has advantages of shortening reaction time,mild conditions and high yield.