- Intermediate compound for preparing 4-chloro-2-trifluoromethyl-acetophenone as well as preparation method and application of intermediate compound
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The invention relates to an intermediate compound for preparing 4-chloro-2-trifluoromethyl-acetophenone as well as a preparation method and application of the intermediate compound. The intermediate compound is 2-(4-chloro-2-(trifluoromethyl) benzoyl) malonate, 3, 4-dimethylchlorobenzene is taken as an initial raw material, and the intermediate compound is obtained by chlorination, fluorine-chlorine exchange reaction, hydrolysis, continuous chlorination and coupling with malonate. The intermediate compound 2-(4-chloro-2-(trifluoromethyl) benzoyl) malonate is subjected to hydrolysis decarboxylation to obtain 4-chloro-2-trifluoromethyl-acetophenone, the raw materials in the route are easy to obtain, dangerous reactions such as nitration and Grignard reaction are avoided, and the method is suitable for industrial production.
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- 2-benzoyl malonate compound as well as preparation method and application thereof
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The invention discloses a 2-benzoyl malonate compound as well as a preparation method and application thereof. The invention provides a preparation method of an acetylbenzene compound shown as a formula III. The preparation method comprises the following step: in an organic solvent, in the presence of an acid and water, carrying out a deesterification reaction as shown in the specification on a 2-benzoyl malonate compound as shown in a formula I and/or a tautomer thereof to obtain the acetylbenzene compound as shown in a formula III, wherein X is F, Cl, Br or I; wherein R1 and R2 are each independently a C1-C4 alkyl group. By adopting the 2-benzoyl malonate compound disclosed by the invention, 4-halogenated-2-trifluoromethyl acetophenone can be prepared through one-step reaction, and the operation is simple and convenient.
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Paragraph 0098; 0102-0104
(2020/07/15)
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- Pyrrolo(oxo)isoquinolines as 5HT ligands
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The present application describes compounds according to Formula I, pharmaceutical compositions, comprising at least one compound according to Formula I and optionally at least one additional therapeutic agent and methods of treating various diseases, conditions and disorders associated with modulation of serotonin receptors such as, for example: metabolic diseases, which includes but is not limited to obesity, diabetes, diabetic complications, atherosclerosis, impared glucose tolerance and dyslipidemia; central nervous system diseases which includes but is not limited to, anxiety, depression, obsessive compulsive disorder, panic disorder, psychosis, schizophrenia, sleep disorder, sexual disorder and social phobias; cephalic pain; migraine; and gastrointestinal disorders using compounds according to Formula I or pharmaceutically acceptable salt forms thereof, wherein A, B, D, E, m, n, R3, R7, R8, R9, R10, R11 and X are described herein.
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Page/Page column 42
(2008/06/13)
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