- Preparation method of ziprasidone intermediate
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The invention relates to a preparation method of a ziprasidone intermediate.The preparation method is a method to prepare 6-chloro-2-indolone by one-pot process, an alkali liquid and phase-transfer catalyst low in price are used in the preparation process to substitute the prior art sodium hydride necessary to use and high in price, recyclable low-grade aliphatic ketone and low-grade fatty alcohol are used to substitute DMF (dimethyl formamide) and DMSO (dimethylsulfoxide) difficult to recycle, the cost is reduced greatly, the materials used herein are cheap and easy to obtain, the process is simple and feasible, posttreatment steps are simplified, particularly the step (1) requires no washing, extracting and purifying operation, one step may be performed directly, the whole operating step needs no use of column chromatography for purification, the whole preparation process is simplified, and the method is convenient to industrialize; in the synthetic process of formula III compound, a deacidifying process is mild and safe; in the synthesis of formula II compound, low-valence sulfur-containing compound is used in reduction, generation of mass waste acid liquid is avoided, production is safe and environment-friendly, and the preparation process is simple and easy.
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Paragraph 0044
(2016/12/01)
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- An aminoisoflavone-salicyloylindole ring transformation
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A series of 2′-nitroisoflavones 8-10, 15, 22, 27 and 28 was prepared via the (2-nitro-phenyl)-acetic acids 1, 13, 19 and 25. In order to obtain the corresponding 2′-aminoisoflavones the reduction of 8-10, 15, 22, 27 and 28 was undertaken. Surprisingly, new 3-salicyloylindoles instead of the expected 2′-aminoisoflavones were the main reduction products. In the following paper the preparation of the 2′-nitroisoflavones 8-10, 15, 22, 27 and 28 as well as the reduction experiments obtaining the 2′-aminoisoflavones 33 and 35 and the 3-salicyloylindoles 29-32, 34 and 36 will be described. Furthermore, a possible mechanism responsible for the formation of the 3-salicyloylindoles from 2′-nitroisoflavones under reductive conditions will be discussed.
- Loewe, Werner,Witzel, Sonja,Tappmeyer, Silvia,Albuschat, Rica
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p. 317 - 326
(2007/10/03)
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- A PROCESS FOR THE PREPARATION OF OXINDOLE DERIVATIVES
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A process for the preparation of oxindole derivative of formula (I) comprising reacting compound of formula (II) with dialkyl malonate, COOR1-COOR1, in the presence of a mild base to give compound of formula (III); and wherein R is selected from hydrogen, linear, branched or cyclic alkyl, aryl, substituted aryl, heteroaryl, haloalkyl like CF3, alkoxy, haloalkoxy, thioalkyl and halogen.; R1 is selected from linear, branched and cyclic alkyl (C1 to C4 groups); and X is selected from chloro, bromo, fluoro and iodo groups;further converting compound of formula (III) to compound of formula (I).
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- Oxindoles as sleep-inducers
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Sleep inducers of the formula: STR1 wherein R is hydrogen or halo of atomic weight of from 18 to 36, R' is hydrogen, halo or CF3 and R° is hydrogen or lower alkyl. Preparation by cyclizing a 2-nitro-phenylacetic acid is also disclosed.
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