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【结 构 式】 
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【分子编号】32910 【品名】di(tert-butyl) 4,6-dichloro-3-formyl-1H-indole-1,2-dicarboxylate 【CA登记号】 |
【 分 子 式 】C19H21Cl2NO5 【 分 子 量 】414.28488 【元素组成】C 55.09% H 5.11% Cl 17.12% N 3.38% O 19.31% |
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：(XI)GV217828 was prepared following the synthetic route shown in Scheme 22578902a. In this event, due to the lability of the cyclic imide in basic medium, indole aldehyde (I) was transformed into the corresponding tert-butyl ester derivative (XI). Wittig reaction with phosphorane (XII) gave the olefinic intermediate (XIII) as a single E regioisomer. The removal of the tert-butyl protecting group afforded the desired compound G-217828 in high yield.
| 【1】 Hedaya, E.; Theodoropulos, S.; Preparation and reactions of stable phosphorus ylides derived from malic anhydrides. Tetrahedron 1968, 24, 2241. |
| 【2】 Di Fabio, R.; Corsi, M.; Ugolini, A.R.; Gaviraghi, G.; Giacobbe, S.; Gastaldi, P.; Pentassuglia, G.; Quartaroli, M.; Conti, N.; Donati, D.; Trist, D.G.; Ratti, E.; GV196771. Drugs Fut 2000, 25, 2, 137. |
| 中间体序号 | 中间体编号 | 品名 | CAS号 | 分子式 | 供应商 | 用于合成 |
|---|---|---|---|---|---|---|
| 21059 | N-[di(tert-butoxy)methyl]-N,N-dimethylamine; di(tert-butoxy)-N,N-dimethylmethanamine | 36805-97-7 | C11H25NO2 | 详情 | 详情 | |
| (I) | 32144 | ethyl 4,6-dichloro-3-formyl-1H-indole-2-carboxylate | C12H9Cl2NO3 | 详情 | 详情 | |
| (IX) | 32906 | 4,6-dichloro-3-formyl-1H-indole-2-carboxylic acid | C10H5Cl2NO3 | 详情 | 详情 | |
| (X) | 32909 | tert-butyl 4,6-dichloro-3-formyl-1H-indole-2-carboxylate | C14H13Cl2NO3 | 详情 | 详情 | |
| (XI) | 32910 | di(tert-butyl) 4,6-dichloro-3-formyl-1H-indole-1,2-dicarboxylate | C19H21Cl2NO5 | 详情 | 详情 | |
| (XII) | 32907 | 5-oxo-1-phenyl-4-(triphenylphosphonio)-4,5-dihydro-1H-pyrrol-2-olate | C28H22NO2P | 详情 | 详情 | |
| (XIII) | 32908 | di(tert-butyl) 4,6-dichloro-3-[(2,5-dioxo-1-phenyl-3-pyrrolidinylidene)methyl]-1H-indole-1,2-dicarboxylate | C29H28Cl2N2O6 | 详情 | 详情 |
Extended Information