P32/98
P32/98(半富马酸盐) Chemical Name: 2(S)-Amino-3(S)-methyl-1-(3-thiazolidinyl)pentan-1-one fumarate; 3-(L-Isoleucyl)thiazolidine fumarate; 3-[2(S)-Amino-3(S)-methylpentanoyl]thiazolidine fumarate
CAS No. 251572-70-0, 136259-20-6 (free base), 140233-53-0 (HCl), 251572-86-8 (hemifumarate), 251571-89-8 (monoacetate), 251573-34-9 (monosulfate), 251573-02-1 (phosphate(1:1)), 251573-50-9 (sulfate salt(2:1))
项目整合开发状态: Phase II
项目研究机构: Probiodrug (Originator), Merck & Co. (Licensee)
合成路线:The condensation of N-(tert-butoxycarbonyl)-L-isoleucine (I) with thiazolidine (II) by means of isobutyl chloroformate and N-ethylmorpholine (NEM) in THF gives 3-[N-(tert-butoxycarbonyl)-L-isoleucyl]thiazolidine (III),which is deprotected with HCl and thioanisole in acetic acid.
📌 参考资料/链接：
参考文献标题:Process for the preparation of new dipeptidyl peptidase IV inhibitors
文献作者:Faust,J.; Heins,J.; Rahfeld,J.U.; Demuth,H.-U.; Steinmetzer,T.; Born,I.; Barth,A.; Neubert,K.(Martin Luther Universit鋞 Halle-Wittenberg)
参考来源:DD 296075
📄 详细内容
合成路线:The condensation of N-(tert-butoxycarbonyl)-L-isoleucine (I) with thiazolidine (II) by means of isobutyl chloroformate and N-ethylmorpholine (NEM) in THF gives 3-[N-(tert-butoxycarbonyl)-L-isoleucyl]thiazolidine (III),which is deprotected with HCl and thioanisole in acetic acid.
参考文献标题:Dipeptidyl peptidase IV in the immune system.Effects of specific enzyme inhibitors on activity of dipeptidyl peptidase IV and proliferation of human lymphocytes
文献作者:Sch鰊,E.; Born,I.; Demuth,H.-U.; faust,J.; Neubert,K.; Steinmetzer,T.; Barth,A.; Ansorge,S.
参考来源:Biol Chem Hoppe Seyler 1991,372(5),305
合成路线:The condensation of N-(tert-butoxycarbonyl)-L-isoleucine (I) with thiazolidine (II) by means of isobutyl chloroformate and N-ethylmorpholine (NEM) in THF gives 3-[N-(tert-butoxycarbonyl)-L-isoleucyl]thiazolidine (III),which is deprotected with HCl and thioanisole in acetic acid.
参考文献标题:P32/98
文献作者:Sorbera,L.A.; Revel,L.; Castar,J.
参考来源:Drugs Fut 2001,26(9),859
产品链接: CAS No.136259-20-6››