DAPT, LY-374973, AN-37124
(2S)-N-[N-(3,5-二氟苯乙酰基)-L-丙氨酰]-2-苯基甘氨酸叔丁酯Chemical Name: N-[2-(3,5-Difluorophenyl)acetyl]-L-alanyl-L-(2-phenyl)glycine tert-butyl ester
CAS No. 208255-80-5
项目整合开发状态: Preclinical
项目研究机构: Elan (Originator), Lilly (Originator)
合成路线:The reaction of 3,5-difluorophenylacetic acid (I) with oxalyl chloride and DMF in dichloromethane gives the corresponding acyl chloride (II),which is condensed with L-alanine (III) by means of aqueous NaOH,yielding N-(3,5-difluorophenylacetyl)-L-alanine (IV).Finally,this compound is condensed with L-phenylglycine tert-butyl ester (V) by means of 2-ethoxy-1,2-dihydroquinoline-1-carboxylic acid ethyl ester (EEDQ) and NMM in THF.
📌 参考资料/链接：
参考文献标题:Methods and cpds.for inhibiting beta-amyloid peptide release and/or its synthesis
文献作者:Porter,W.J.; Eid,C.N.; Audia,J.E.; Britton,T.C.; Latimer,L.H.; Droste,J.J.; Scott,W.L.; Wu,J.; Tung,J.S.; Thorsett,E.D.; John,V.; Huffman,G.W.; (Athena Neurosciences,Inc.; Eli Lilly and Company)
参考来源:JP 2001503782; WO 9822494