【结 构 式】 |
【分子编号】46947 【品名】2-[2-(2-bromo-1H-indol-3-yl)ethyl]-1H-isoindole-1,3(2H)-dione 【CA登记号】 |
【 分 子 式 】C18H13BrN2O2 【 分 子 量 】369.2175 【元素组成】C 58.56% H 3.55% Br 21.64% N 7.59% O 8.67% |
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:(II)Bromination of N-phthaloyl tryptamine (I) with pyridinium tribromide provided the 2-bromo indole (II). Suzuki coupling of bromide (II) with phenylboronic acid (III) gave the 2-phenyl indole (IV). The phthaloyl group of (IV) was then removed by treatment with dimethylamine to furnish 2-phenyltryptamine (V). Then condensation of amine (V) with 3-methyl-2-oxovaleric acid (VI) using EDC and HOBt yielded the corresponding amide.
【1】 Viziano, M.; Seneci, P.; Michelli, F.; Cavallini, P.; Zumerle, A.; Kennedy, G.; Winders, J.A.; Gevi, M.; Rodegher, P.; Studies on the novel anti-staphyloccal compound nematophin. Bioorg Med Chem Lett 2000, 10, 15, 1751. |
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) | 46946 | 2-[2-(1H-indol-3-yl)ethyl]-1H-isoindole-1,3(2H)-dione | C18H14N2O2 | 详情 | 详情 | |
(II) | 46947 | 2-[2-(2-bromo-1H-indol-3-yl)ethyl]-1H-isoindole-1,3(2H)-dione | C18H13BrN2O2 | 详情 | 详情 | |
(III) | 16593 | Phenylboronic acid;Benzeneboronic acid;Phenylboron dihydroxide | 98-80-6 | C6H7BO2 | 详情 | 详情 |
(IV) | 46948 | 2-[2-(2-phenyl-1H-indol-3-yl)ethyl]-1H-isoindole-1,3(2H)-dione | C24H18N2O2 | 详情 | 详情 | |
(V) | 46949 | 2-(2-phenyl-1H-indol-3-yl)-1-ethanamine; 2-(2-phenyl-1H-indol-3-yl)ethylamine | C16H16N2 | 详情 | 详情 | |
(VI) | 46950 | 3-methyl-2-oxopentanoic acid | C6H10O3 | 详情 | 详情 |
Extended Information