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【结 构 式】

【分子编号】30008

【品名】tert-butyl (1S)-2-methyl-1-(1,3-thiazolidin-3-ylcarbonyl)butylcarbamate

【CA登记号】

【 分 子 式 】C14H26N2O3S

【 分 子 量 】302.43812

【元素组成】C 55.6% H 8.67% N 9.26% O 15.87% S 10.6%

与该中间体有关的原料药合成路线共 1 条

合成路线1

该中间体在本合成路线中的序号:(III)

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 .
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(I) 30009 (2S,3S)-2-[(tert-butoxycarbonyl)amino]-3-methylpentanoic acid 13139-16-7 C11H21NO4 详情 详情
(II) 28093 1,3-thiazolidine 504-78-9 C3H7NS 详情 详情
(III) 30008 tert-butyl (1S)-2-methyl-1-(1,3-thiazolidin-3-ylcarbonyl)butylcarbamate C14H26N2O3S 详情 详情
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