- Use of a modified Leimgruber-Batcho reaction to prepare 6-chloro-5-fluoroindole
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An efficient synthesis of the title indole, the heterocyclic core of the standard 5-HT2C receptor agonist Ro 60-0175, via a modified Leimgruber-Batcho indole synthesis is presented. The process can be used to make > 100 g quantities of the targ
- Bentley, Jon M.,Davidson, James E.,Duncton, Matthew A. J.,Giles, Paul R.,Pratt, Robert M.
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- Preparation method of 2,4,5-trifluorophenylacetic acid
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The invention belongs to the technical field of preparation of drug intermediates, and discloses a preparation method of 2,4,5-trifluorophenylacetic acid, wherein the preparation method comprises the steps: step 1, reacting raw materials, a quaternary ammonium salt catalyst, sulfolane and potassium fluoride to obtain a first intermediate; step 2, carrying out hydrogenation catalytic reaction on the first intermediate to obtain a second intermediate; step 3, carrying out salt forming reaction on the second intermediate and a fluorinating reagent, quenching, and carrying out diazotization reaction on the second intermediate and a sodium nitrite aqueous solution to obtain diazonium salt; step 4, carrying out high-temperature cracking on the diazonium salt, to obtain 2,4,5-trifluorotoluene; and step 5 to step 7, carrying out halogenation, cyanidation and hydrolysis reactions on 2,4,5-trifluorotoluene in sequence, and thus obtaining 2,4,5-trifluorophenylacetic acid. The raw materials adopted by the method are easy to obtain and low in cost, the yield of the corresponding product obtained in each step is high, and large-scale production of the 2,4,5-trifluorophenylacetic acid is facilitated.
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Paragraph 0040
(2021/05/29)
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- ANTITUMOR-EFFECT ENHANCER USING PYRAZOLO[3,4-D]PYRIMIDINE COMPOUND
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To provide a method for treating cancer using a pyrazolo[3,4-d]pyrimidine compound or a salt thereof. The present invention provides an antitumor agent comprising a pyrazolo[3,4-d]pyrimidine compound of formula (I) wherein X, Y, Z1, Z2/su
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Paragraph 0361
(2020/01/22)
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- NOVEL PYRAZOLO[3,4-d]PYRIMIDINE COMPOUND OR SALT THEREOF
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To provide a novel compound having a HER2 inhibitory effect and having a cytostatic effect. It is also intended to provide a medicament useful in the prevention and/or treatment of a disease involving HER2, particularly, cancer, on the basis of the HER2 i
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Paragraph 0417
(2017/08/26)
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- Indoline derivatives as 5-HT2C receptor agonists
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A series of 1-(1-indolinyl)-2-propylamines was synthesised and evaluated as 5-HT2C receptor agonists for the treatment of obesity. The general methods of synthesis of the precursor indoles are described. The functional efficacy and radioligand
- Bentley,Adams,Bebbington,Benwell,Bickerdike,Davidson,Dawson,Dourish,Duncton,Gaur,George,Giles,Hamlyn,Kennett,Knight,Malcolm,Mansell,Misra,Monck,Pratt,Quirk,Roffey,Vickers,Cliffe
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p. 2367 - 2370
(2007/10/03)
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- Indoline derivatives as 5-HT2B and or 5-HTC receptor ligands
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For use in therapy a chemical compound of formula (I), wherein R1to R3are independently selected from hydrogen and alkyl; R4to R7are independently selected from hydrogen, halogen, hydroxy, alkyl, aryl, heterocyclyl, alkoxy, aryloxy, alkylthio, arylthio, alkylsulfoxyl, alkylsulfonyl, arylsulfoxyl, arylsulfonyl, amino, monoalkylamino, dialkylamino, nitro, cyano, carboxaldehyde, alkylcarbonyl, arylcarbonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, alkoxycarbonylamino, aminocarbonyloxy, monoalkylaminocarbonyloxy, dialkylaminocarbonyloxy, monoalkylaminocarbonylamino and dialkylaminocarbonylamino, wherein at least one of R4to R7is a substituent group other than hydrogen, and pharmaceutically acceptable salts and prodrugs thereof, particularly for the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes insipidus, and sleep apnea, and especially for the treatment of obesity; chemical compounds of formula (I) other than compounds wherein R7is hydroxy.
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