药物详细合成路线
| Name | Tropisetron;ICS-205930;Novaban;Navoban | | Chemical Name | 1H-Indole-3-carboxylic acid 3alpha-tropanyl ester
1H-Indole-3-carboxylic acid endo-8-methyl-8-azabicyclo[3.2.1]oct-3-yl ester | | CAS | 89565-68-4 | | Related CAS | 105826-92-4 (HCl) | | Formula | C17H20N2O2 | | Structure |  | | Formula Weight | 284.36115 | | Stage | 上市-1992 | | Company | Novartis (Originator), Asta Medica (Licensee), Kyowa Hakko (Licensee) | | Activity/Mechanism | Fibromyalgia, Treatment of, Nausea and Vomiting, Treatment of, NEUROLOGIC DRUGS, Neurologic Drugs (Miscellaneous), Sensation Disorders, Treatment of, 5-HT3 Antagonists | | Syn. Route | 1 | | Route 1 | | by condensation of indole 3-carbonyl chloride (i) with endo-8-methyl-8-azabicyclo[3.2.1]octan-3-ol (ii) by means of butyllithium in thf, or na2co3 in the same solvent. | | |  | | List of intermediates | No. | | 2,2,2-trichloroethyl 4-[(2r)-2-([[(1s,2r,3s)-1-(cyclohexylmethyl)-2,3-dihydroxy-5-methylhexyl]amino]carbonyl)-4-[(cyclohexylmethyl)(2-[methyl[2-(2-pyridinyl)ethyl]amino]-2-oxoethyl)amino]-4-oxobutyl]-1,3-thiazol-2-ylcarbamate | (i) | | o-toluquinoline; 8-methylquinoline | (ii) | | | Reference 1: donatsch, p.; engel, g.; stadler, p.; richardson, b.p.; hügi, b. (novartis ag; novartis deutschland gmbh); pharmaceutically useful heterocyclic and carbocyclic acid esters and amides of alkylene bridged piperidines. ch 669792; ch 669954; de 3322574; gb 2166726; gb 2166727; gb 2166728; us 4789673 . Reference 2: castaner, j.; serradell, m.n.; ics-205930. drugs fut 1986, 11, 2, 106. |
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来源:药化网
作者:药化小编
摘要:本文合成路线介绍的是药物中文名托烷司琼；英文名Tropisetron;ICS-205930;Novaban;Navoban；CAS[89565-68-4]
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