SU-740(non-complexed), SU-840
Chemical Name: 4-tert-Butyl-2'-(carboxymethoxy)-4'-(3-methyl-2-butenyloxy)chalcone beta-cyclodextrin complex; (E)-2-[2-(4-tert-Butylcinnamoyl)-5-(3-methyl-2-butenyloxy)phenoxy]acetic acid beta-cyclodextrin complex
CAS No. 134336-72-4 (noncomplexed)
项目整合开发状态: Preclinical
项目研究机构: Taisho (Originator)
合成路线:The synthesis of free compound is performed as follows:The condensation of 2-hydroxy-4-(3-methyl-2-butenyloxy)acetophenone (I) with 4-tert-butylbenzaldehyde (II) by means of KOH in hot ethanol gives 3-(4-tert-butylphenyl)-1-[4-hydroxy-4-(3-methyl-2-butenyloxy)phenyl]-2(E)-propen-1-one (III),which is condensed with ethyl bromoacetate (IV) by means of KOH in acetone to afford (E)-2-[2-(4-tert-butylcinnamoyl)-4-(3-methyl-2-butenyloxy)phenoxy] acetic acid ethyl ester (V).Finally,this compound is hydrolyzed with KOH in hot ethanol-water.
📌 参考资料/链接:
参考文献标题:Chalcone derivs
文献作者:Yokomori,S.; Saijo,K.; Matsunaga,T.; Nakashima,Y.; Hatayama,K.(Taisho Pharmaceutical Co.,Ltd.)
参考来源:EP 0412803; JP 1991163042
📄 详细内容
合成路线:The synthesis of free compound is performed as follows:The condensation of 2-hydroxy-4-(3-methyl-2-butenyloxy)acetophenone (I) with 4-tert-butylbenzaldehyde (II) by means of KOH in hot ethanol gives 3-(4-tert-butylphenyl)-1-[4-hydroxy-4-(3-methyl-2-butenyloxy)phenyl]-2(E)-propen-1-one (III),which is condensed with ethyl bromoacetate (IV) by means of KOH in acetone to afford (E)-2-[2-(4-tert-butylcinnamoyl)-4-(3-methyl-2-butenyloxy)phenoxy] acetic acid ethyl ester (V).Finally,this compound is hydrolyzed with KOH in hot ethanol-water.
参考文献标题:Antiulcerative agents
文献作者:Yokomori,S.; Saijo,K.; Hatayama,M.(Taisho Pharmaceutical Co.,Ltd.)
参考来源:JP 1993058885
合成路线:The synthesis of free compound is performed as follows:The condensation of 2-hydroxy-4-(3-methyl-2-butenyloxy)acetophenone (I) with 4-tert-butylbenzaldehyde (II) by means of KOH in hot ethanol gives 3-(4-tert-butylphenyl)-1-[4-hydroxy-4-(3-methyl-2-butenyloxy)phenyl]-2(E)-propen-1-one (III),which is condensed with ethyl bromoacetate (IV) by means of KOH in acetone to afford (E)-2-[2-(4-tert-butylcinnamoyl)-4-(3-methyl-2-butenyloxy)phenoxy] acetic acid ethyl ester (V).Finally,this compound is hydrolyzed with KOH in hot ethanol-water.
参考文献标题:SU-840
文献作者:Rabasseda,X.; Castar,J.; Mealy,N.
参考来源:Drugs Fut 1994,19(10),923