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【结 构 式】

【分子编号】29472

【品名】di(tert-butyl) (2S)-2-[[(4-nitrophenoxy)carbonyl]amino]pentanedioate

【CA登记号】

【 分 子 式 】C20H28N2O8

【 分 子 量 】424.451

【元素组成】C 56.6% H 6.65% N 6.6% O 30.16%

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 reaction of L-glutamic acid di tert-butyl ester (I) with 4-nitrophenyl chloroformate (II) by means of triethylamine in dichloromethane gives the corresponding carbamate (III), which is treated with 4-methoxythiophenol (IV) in dichloromethane to afford the thiocarbamate (V). Finally, this compound is treated with HCl.

1 Browne, P.J.; Burke, P.J.; Eno-Amooquaye, E.A.; Khan, T.H.; Osborn, H.M.I.; Searle, F.; Novel inhibitors of carboxypeptidase G2 (CPG2): Potential use in antibody-directed enzyme prodrug therapy. J Med Chem 1999, 42, 6, 951.
2 Khan, T. (Aepact Ltd.); Drug therapy. WO 9720580 .
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) 29471 di(tert-butyl) (2S)-2-aminopentanedioate C13H25NO4 详情 详情
(II) 16605 4-Nitrophenyl chloroformate; 1-[(Chlorocarbonyl)oxy]-4-nitrobenzene 7693-46-1 C7H4ClNO4 详情 详情
(III) 29472 di(tert-butyl) (2S)-2-[[(4-nitrophenoxy)carbonyl]amino]pentanedioate C20H28N2O8 详情 详情
(IV) 25639 4-methoxyphenylhydrosulfide; 4-methoxybenzenethiol 34320-82-6 C7H8OS 详情 详情
(V) 29473 di(tert-butyl) (2S)-2-([[(4-methoxyphenyl)sulfanyl]carbonyl]amino)pentanedioate C21H31NO6S 详情 详情
Extended Information