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【结 构 式】

【分子编号】55378

【品名】5-[1,3-dioxo-1H-benzo[de]isoquinolin-2(3H)-yl]isophthalic acid

【CA登记号】

【 分 子 式 】C20H11NO6

【 分 子 量 】361.31048

【元素组成】C 66.49% H 3.07% N 3.88% O 26.57%

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 5-aminoisophthalic acid (I) with 1,8-naphthalic anhydride (II) in DMSO/pyridine gives the expected naphthalimide (III), which is condensed with diethylenetriamine (IV) by means of CDI in DMA to yield the isophthalamide (V). Finally, the free amino groups of (V) are condensed with 4-chloronaphthalic anhydride (VI) in pyridine/DMSO to afford the target tris naphthalimide.

1 Suzuki, K.; Yamada, Y.; Asao, T.; Noguchi, K.; Wakida, M. (Taiho Pharmaceutical Co., Ltd.); Naphthalimidobenzamide derivs.. EP 1020446; US 6300331; WO 0001672 .
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) 55377 5-Aminobenzene-1,3-dicarboxylic acid; 5-Aminoisophthalic acid; 5-Aminoisophthalmic acid 99-31-0 C8H7NO4 详情 详情
(II) 16982 1H,3H-benzo[de]isochromene-1,3-dione; 1,8-Naphthalic Anhydride 81-84-5 C12H6O3 详情 详情
(III) 55378 5-[1,3-dioxo-1H-benzo[de]isoquinolin-2(3H)-yl]isophthalic acid C20H11NO6 详情 详情
(IV) 55379 2,2'-Diaminodiethylamine; 2,2'-Iminodiethylamine; Bis(beta-Aminoethyl)amine; Diethylentriamine; N-(2-Aminoethyl)-1,2-ethanediamine 111-40-0 C4H13N3 详情 详情
(V) 55380 N~1~,N~3~-bis{2-[(2-aminoethyl)amino]ethyl}-5-[1,3-dioxo-1H-benzo[de]isoquinolin-2(3H)-yl]isophthalamide C28H33N7O4 详情 详情
(VI) 55381 4-Chloro-1,8-naphthalic anhydride 4053-08-1 C12H5ClO3 详情 详情
Extended Information