PPYDC

Chemical Name: (1S,2R)-2-[1(R)-Amino-2-propynyl]-N,N-diethyl-1-phenylcyclopropanecarboxamide hydrochloride
项目整合开发状态: Biological Testing
项目研究机构: Hokkaido University (Originator), Kyushu Institute of Technology (Originator)
合成路线:Addition of lithium trimethylsilylacetylide (II) to chiral cyclopropane- carbaldehyde (I) gave propargyl alcohol (III).This was condensed with NaN3 in the presence of CBr4 and PPh3 to provide azide (IV) with retention of configuration.Subsequent treatment of (IV) with PPh3 in pyridine,and then with aqueous ammonia furnished the desired amine,which was isolated as the hydrochloride salt after chromatography over Diaion WA-30 resin.
📌 参考资料/链接:
参考文献标题:Synthesis and biological activity of conformationally restricted analogues of milnacipran: (1S,2R)-1-phenyl-2-[(R)-1-amino-2-propynyl]-N,N-diethylcyclopropanecarboxamide is a novel class of NMDA receptor channel blocker
文献作者:Shuto,S.; Ono,S.; Imoto,H.; Yoshii,K.; Matsuda,A.
参考来源:J Med Chem 1998,41(18),3507