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【结 构 式】 
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【药物名称】P32/98 【化学名称】2(S)-Amino-3(S)-methyl-1-(3-thiazolidinyl)pentan-1-one fumarate 【CA登记号】251572-70-0, 136259-20-6 (free base), 140233-53-0 (HCl), 251572-86-8 (hemifumarate), 251571-89-8 (monoacetate), 251573-34-9 (mon 【 分 子 式 】C13H22N2O5S 【 分 子 量 】318.39469 |
【开发单位】Probiodrug (Originator), Merck & Co. (Licensee) 【药理作用】Antidiabetic Drugs, ENDOCRINE DRUGS, Type 2 Diabetes Mellitus, Agents for, Dipeptidyl-Peptidase IV Inhibitors, Insulin Secretagogues, Prolyl Endopeptidase (prolyl oligopeptidase; POP) Inhibitors |
合成路线1
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.
| 【1】 Sorbera, L.A.; Revel, L.; Castañer, J.; P32/98. Drugs Fut 2001, 26, 9, 859. |
| 【2】 Born, I.; Barth, A.; Ansorge, S.; faust, J.; Neubert, K.; Schön, E.; Steinmetzer, T.; Demuth, H.-U.; Dipeptidyl peptidase IV in the immune system. Effects of specific enzyme inhibitors on activity of dipeptidyl peptidase IV and proliferation of human lymphocytes. Biol Chem Hoppe Seyler 1991, 372, 5, 305. |
| 【3】 Faust, J.; Heins, J.; Rahfeld, J.U.; Demuth, H.-U.; Steinmetzer, T.; Born, I.; Barth, A.; Neubert, K. (Martin Luther Universitat Halle-Wittenberg); Process for the preparation of new dipeptidyl peptidase IV inhibitors. DD 296075 . |