855382-76-2Relevant academic research and scientific papers
A process for preparing 4 - (2 - hydroxyethyl) - 1, 3 - dihydro - 2H - indole -2 - one of the new method
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Paragraph 0050-0053, (2019/04/04)
The invention discloses a novel method for preparing a ropinirole hydrochloride key intermediate 4-(2-ethoxy)-1,3-dihydro-2H-indole-2-ketone (I). The reaction process comprises the following steps of: carrying out reduction reaction on 2-methyl-3-nitrobenzene acetic acid (III) to generate 2-methyl-3-nitrobenzene ethanol (IV); protecting the hydroxyl of the compound (IV) to generate 2-methyl-3-(2-alkoxy ethyl) nitrobenzene (V); reacting the compound (V) with diethyl oxalate to generate a 2-nitro-6-(2-alkoxy ethyl)-phenyl acetyl formic acid compound (VI); reacting the compound (VI) with hydrogen peroxide to generate 2-nitro-6-(2-alkoxy ethyl)-phenylacetic acid (VII); and carrying out oxidation reaction on the compound (VII) to obtain 4-(2-ethoxy)-1,3-dihydro-2H-indole-2-ketone (I).
A convenient synthesis of 4-(2-hydroxyethyl)indolin-2-one, a useful intermediate for the preparation of both dopamine receptor agonists and protein kinase inhibitors
Matera, Carlo,Quadri, Marta,Pelucchi, Silvia,De Amici, Marco,Dallanoce, Clelia
, p. 1139 - 1144 (2014/06/24)
This paper describes a practical approach to the preparation of 4-(2-hydroxyethyl)indolin-2-one, a key intermediate in the synthesis of dopaminergic agonists such as ropinirole - a drug used in the treatment of Parkinson's disease and restless legs syndrome - and of two sets of protein kinase inhibitors. The sequence starts from commercially available 2-(2-methyl-3-nitrophenyl)acetic acid, which is converted in five steps into the desired target compound. This procedure offers a convenient alternative route to existing methodologies, given its milder reaction conditions, ease of implementation, and its overall yield (59 %).
A new scalable route to 4-(2-hydroxyethyl)-1,3-dihydro-2 H-indol-2-one: A key intermediate for ropinirole hydrochloride
Chen, Huansheng,Chen, Yu,Yuan, Li,Zou, Qing
, p. 714 - 717 (2013/06/27)
A new and efficient manufacturing technology is disclosed in the present work for the preparation of 4-(2-hydroxyethyl)-1,3-dihydro-2H-indol-2-one, which is a key intermediate for ropinirole hydrochloride. The whole process gives the target molecule in 71% overall yield with 99% purity. In the final step, a novel nitro reduction/ring-closing/debenzylation takes place in one pot. All the intermediates can be used directly for the next step without purification in this process.
Benzazepine Compound
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Page/Page column 24, (2011/11/12)
[Problem] Provided is a compound which is useful as an agent for treating or preventing 5-HT2C receptor-related diseases, particularly incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and
PROCESS FOR THE PREPARATION OF INDOLONE DERIVATIVE
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Page/Page column 23, (2008/06/13)
A process for the preparation of 4-[2-(Di-n-propylamino) ethyl]-2,3-dihydro-1 H-indol-2-one of formula (I) and its pharmaceutically acceptable salts, solvates Formaula I involving new intermediates of compound of formula (A) and (B) wherein R represents (i) a halogen atom selected from fluorine, chlorine atom, bromine atom and iodine atom; (ii) lower alkanesulfonyloxy group selected from methanesulfonyloxy, ethanesulfonyloxy, isopropanesulfonyloxy, propanesulfonyloxy, butanesulfonyloxy, tert-butanesulfonyloxy, pentanesulfonyloxy, hexanesulfonyloxy; (iii) substituted or unsubstantiated arylsulfonyloxy group selected from phenylsulfonyloxy, 4-methylphenylsulfonyloxy, 2-methylphenylsulfonyloxy, 4- nitrophenylsulfonyloxy, 4- methoxyphenylsulfonyloxy, 3-chlorophenylsulfonyloxy; (iv) arylalkylsulfonyloxy group selected from benzylsulfonyloxy, 2- phenylethylsulfonyloxy, 4-phenylbutylsulfonyloxy, 4- methylbenzylsulfonyloxy, 2- methylbenzylsulfonyloxy, 4- nitrobenzylsulfonyloxy, 4-methoxybenzylsulfonyloxy, 3- chlorobenzylsulfonyloxy.
