The invention discloses a preparation method of 3 - (trifluoromethyl) -4 -indolinic acid. The method comprises the following steps: (1) protecting the indole 4 - formic acid through a benzyl protecting carboxylic acid to obtain the compound shown in the formula 1. (2): The compound represented by Formula 1 is protected by an amino group to obtain a compound represented by Formula 2. (3): The compound represented by Formula 2 is substituted with iodine to obtain a compound represented by Formula 3. (4): A compound represented by Formula 3 is mixed with a trifluoromethylation reagent to react to obtain a compound having the structure shown in Formula 4. (5) The compound of formula 4 was subjected to deamination protection and benzyl to give 3 - (trifluoromethyl) -4 -indolinic acid.
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Paragraph 0059-0061; 0072-0073
(2021/09/15)
Discovery and evaluation of a series of 3-acylindole imidazopyridine platelet-activating factor antagonists
Studies conducted with the goal of discovering a second-generation platelet-activating factor (PAF) antagonist have identified a novel class of potent and orally active antagonists which have high aqueous solubility and long duration of action in animal m
Curtin, Michael L.,Davidsen, Steven K.,Heyman, H. Robin,Garland, Robert B.,Sheppard, George S.,Florjancic, Alan S.,Xu, Lianhong,Carrera Jr., George M.,Steinman, Douglas H.,Trautmann, Jeff A.,Albert, Daniel H.,Magoc, Terrance J.,Tapang, Paul,Rhein, David A.,Conway, Richard G.,Luo, Gongjin,Denissen, Jon F.,Marsh, Kennan C.,Morgan, Douglas W.,Summers, James B.
p. 74 - 95
(2007/10/03)
Synthesis of N-Alkyl Derivatives of 4-(2'-Aminoethyl)indole
N-Substituted 4-(2'-aminoethyl)indoles are attainable in good yields from indole-4-acetic acid (2).Several methods of preparation for 2 were tried or considered.A new sequence involving Arndt-Eistert homologation of indole-4-carboxylic acid has been devis
Cannon, Joseph G.,Demopoulos, Basil J.
p. 1195 - 1199
(2007/10/02)
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