- Synthesis method of 5-bromo-4-methoxy-1H-indazole
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The invention belongs to the field of organic synthesis, and particularly relates to a synthetic method of 5-bromo-4-methoxy-1H-indazole. The synthesis method provided by the invention comprises the following steps: (1) dissolving 4-methoxy-1H-indazole in toluene, heating the component to 70-110 DEG C, adding acetic anhydride, and performing a reaction for 0.5 h to obtain 1-(4-methoxy-1H-indazole-1-yl) ethyl ketone; (2) dissolving 1-(4-methoxy-1H-indazole-1-yl) ethyl ketone into tetrahydrofuran, adding N-bromosuccinimide, stirring the components in an ice bath for 1 hour, and removing the icebath to react for 12 hours, so as to obtain 1-(5-bromo-4-methoxy-1H-indazole-1-yl) ethyl ketone; and (3) dissolving 1-(5-bromo-4-methoxy-1H-indazole-1-yl) ethyl ketone in methanol, then adding ammoniawater, and carrying out a stirring reaction for 1 h so as to obtain 5-bromo-4-methoxy-1H-indazole. The compound provided by the invention can be used as an important drug intermediate, and the synthesis method has the advantages of simple synthesis path, high product yield and the like.
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Paragraph 4-6
(2019/12/02)
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- Substituted Quinazoline and Pyridopyrimidine Derivatives Useful as Anticancer Agents
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Compounds of the general formula: processes for the preparation of these compounds, compositions containing these compounds, and the uses of these compounds.
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Paragraph 0216; 0217
(2019/08/22)
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- BICYCLIC HETEROCYCLES AS BET PROTEIN INHIBITORS
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The present invention relates to bicyclic heterocycles which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.
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Paragraph 0528; 0529
(2015/06/03)
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- ESTROGEN RECEPTOR MODULATORS AND USES THEREOF
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Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
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Paragraph 00492
(2013/10/08)
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- Protective Agent for Retinal Neuronal Cell Comprising Indazole Derivative as Active Ingredient
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As a result of intensive studies for the purpose of finding a new medicinal use of an indazole derivative, it was found that an indazole derivative inhibits glutamate-induced retinal neuronal cell death in rat fetal retinal neuronal cells, in other words, the indazole derivative acts directly on the retinal neuronal cells and exhibits an effect of protecting retinal neuronal cells. Accordingly, the indazole derivative is useful for the prevention or treatment of an eye disease associated with retinal neuronal cell damage or retinal damage.
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Page/Page column 11
(2009/01/23)
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- INDAZOLES USED TO TREAT ESTROGEN RECEPTOR BETA MEDIATED DISORDERS
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The present invention relates to novel indazole derivatives (I) having pharmacological activity, processes for their preparation, compositions containing them and uses of these compounds in the treatment of estrogen receptor beta mediated diseases.
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Page/Page column 25
(2008/12/07)
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- NOVEL INDAZOLE DERIVATIVE
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An object of the present invention is to create a novel indazole derivative useful as a drug and to find a novel pharmacological action of the derivative. The compound of the present invention is represented by the formula [I] and has an excellent Rho kinase inhibiting action. In the formula, a ring X is a benzene ring or a pyridine ring; R1 and R2 are H or alkyl; R3 and R4 are halogen, H, OH, alkoxy, alkenyloxy, alkynyloxy, cycloalkyloxy, cycloalkenyloxy, aryloxy, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, carboxy, hydrocarbonyl, alkylcarbonyl, etc.; and R5 is halogen atom, H, OH, alkoxy, aryloxy, alkyl or aryl. Each group can be substituted.
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Page/Page column 45
(2008/06/13)
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