Thymectacin, NB-1011, NB-101, -Drug Synthesis Database

【结构式】

【药物名称】Thymectacin, NB-1011, NB-101

【化学名称】N-[[5-[(E)-2-Bromovinyl]-2'-deoxyuridin-5'-O-yl](phenoxy)phosphoryl]-L-alanine methyl ester

【CA登记号】232925-18-7

【分子式】C₂₁H₂₅BrN₃O₉P

【分子量】574.3259

【开发单位】NewBiotics (Originator), Elan (Licensee)

【药理作用】Breast Cancer Therapy, Colorectal Cancer Therapy, Head and Neck Cancer Therapy, Oncolytic Drugs, Pancreatic Cancer Therapy

合成路线1

The title compound was synthesized by coupling 5-(bromovinyl)-2'-deoxyuridine (I) with phenyl L-methoxyalanino phosphoroamidate (II) in the presence of imidazole in DMF.

参考文献中间体

【1】 Vaino, A.R.; Lobl, T.J.; Baehr, D.N.; Lehsten, D.M.; An improved procedure for the synthesis of nucleoside phosphoramidates. Org Process Res Dev 2002, 6, 6, 819.
【2】 Shepard, H.M. (NewBiotics, Inc.); Enzyme catalyzed therapeutic agents. EP 1167972; JP 2001220397; US 6245750; WO 9937753 .

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)	49856	5-[(E)-2-bromoethenyl]-1-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)tetrahydro-2-furanyl]-2,4(1H,3H)-pyrimidinedione		C₁₁H₁₃BrN₂O₅	详情	详情
(II)	41417	methyl (2S)-2-[[chloro(phenoxy)phosphoryl]amino]propanoate		C₁₀H₁₃ClNO₄P	详情	详情

Extended Information

Drug NewChemical Entity Original Patent(1)