新产品编号:2305483
Chemical Name: 3-(O-Methylpolyethyleneglycol)propionic acid 3-(1-methyl-1H-indol-3-yl)-4-(1-methyl-6-nitro-1H-indol-3-yl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-1-ylmethyl ester
项目整合开发状态: Preclinical
项目研究机构: Roche (Originator)
合成路线:The reaction of Ro 31-7453 (I) (see scheme no.28721501a) with formaldehyde in water at 125 C gives the N-hydroxymethyl derivative (II),which is esterified with 2-(polyoxyethylenoxy)acetic acid (III) by means of EDC and DMAP in dichloromethane to yield the target prodrug.Alternatively,the target prodrug can also be obtained by condensation of Ro 31-7453 (I) with 2-(polyoxyethylenoxy)acetic acid chloromethyl ester (IV) by means of Cs2CO3 in DMF.
📌 参考资料/链接:
参考文献标题:A water soluble prodrug for Ro 31-7453 suitable for both oral delivery and continuous infusion
文献作者:Liu,E.A.; et al.
参考来源:Proc Am Assoc Cancer Res 2002,43Abst 1040