- Synthesis of 2-Oxindoles from Substituted Indoles by Hypervalent-Iodine Oxidation
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A practical conversion of indoles into the corresponding 2-oxindoles is achieved efficiently using a hypervalent iodine reagent. This oxidation is amenable to different substituted indoles, and allows the synthesis of a wide range of synthetically valuable substituted 2-oxindoles in up to 90 % yield. Furthermore, Ropinirole, a drug used to alleviate the symptoms of Parkinson's disease, was synthesized in three steps in an overall yield of 44 % using this method.
- Jiang, Xinpeng,Zheng, Cong,Lei, Lijun,Lin, Kai,Yu, Chuanming
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p. 1437 - 1442
(2018/04/06)
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- 4-Indolyl-N-hydroxyphenylacrylamides as potent HDAC class I and IIB inhibitors in?vitro and in?vivo
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A series of 4,5-indolyl-N-hydroxyphenylacrylamides, as HDAC inhibitors, has been synthesized and evaluated in?vitro and in?vivo. 4-Indolyl compounds 13 and 17 functions as potent inhibitors of HDAC1 (IC50 1.28?nM and 1.34?nM) and HDAC 2 (ICsub
- Mehndiratta, Samir,Wang, Ruei-Shian,Huang, Han-Li,Su, Chih-Jou,Hsu, Chia-Ming,Wu, Yi-Wen,Pan, Shiow-Lin,Liou, Jing-Ping
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- PROCESS FOR THE PREPARATION OF ROPINIROLE
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A new process for the preparation of Ropinirole (1) and pharmaceutically acceptable hydrochloride salt thereof comprising reacting the compound V with nitromethane to obtain the compound of formula 11, which is reduced to compound III and alkylated to obtain compound IV. The oxidation of the indole ring provides the compound of formula (I).
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Page/Page column 4
(2008/06/13)
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- Azepinoindole derivatives with high affinity for brain dopamine and serotonin receptors
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We synthesized 20 and 21 as conformationally constrained analogues of the dopamine receptor antagonist SKF-83742, as well as analogues 6-9, 16, and 18-22. Although 20 and 21 were inactive, 7, 9, and 19 showed strong binding to D-1, D-2, S-2, and α-1 receptors, as well as antipsychotic activity in vivo.
- Maryanoff, Bruce E.,McComsey, David F.,Martin, Gregory E.,Shank, Richard P.
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p. 983 - 988
(2007/10/03)
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