- Synthesis method of 4-fluoro-7-nitroindole or derivatives of 4-fluoro-7-nitroindole
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The invention is applicable to the technical field of chemical synthesis, and provides a synthesis method of 4-fluoro-7-nitroindole or derivatives thereof, which comprises the following steps: reacting 4-fluoroindole or derivatives thereof, glacial acetic acid and sodium cyanoborohydride to obtain 4-fluoroindoline or derivatives thereof, reacting the 4-fluoroindoline or derivatives thereof, glacial acetic acid and acetic anhydride to obtain N-acetyl-4-fluoroindoline or a derivative thereof, carrying out nitration reaction on N-acetyl-4-fluoroindoline or a derivative thereof to obtain N-acetyl4-fluoro-7-nitroindoline or a derivative thereof, reacting N-acetyl-4-fluorine 7-nitroindoline or derivatives thereof, sodium hydroxide and 1, 4-dioxane to obtain 4-fluoro-7-nitroindoline or derivatives thereof, and reacting 4-fluoro-7-nitroindoline or derivatives thereof, trichloromethane and manganese dioxide to obtain 4-fluoro-7-nitroindoline or derivatives thereof. The synthesis method provided by the invention is mild in reaction condition and easy to operate.
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- 5-SULFAMOYL-2-HYDROXYBENZAMIDE DERIVATIVES
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The invention is directed to substituted salicylamide derivatives. Specifically, the invention is directed to compounds according to Formula (I): wherein R, R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof. The compounds of the invention are inhibitors of CD73 and can be useful in the treatment of cancer, pre-cancerous syndromes and diseases associated with CD73 inhibition, such as AIDS, the treatment of HIV, autoimmune diseases, infections, atherosclerosis, and ischemia–reperfusion injury. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting CD73 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
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- PYRROLE ANTIFUNGAL AGENTS
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The invention provides compounds of formula (I), and pharmaceutically and agriculturally acceptable salts thereof; wherein: R1, R2, R3, R4, R5, R6, A1, L1 and n are as defined herein. These compounds and their pharmaceutically acceptable salts are useful in prevention or treatment of a fungal disease. Compounds of formula (I), and agriculturally acceptable salts thereof, may also be used as agricultural fungicides.
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- N-SUBSTITUTED PIPERIDINE AND PIPERAZINE DERIVATIVES
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This invention relates to compounds of the formula 1 wherein R1, R2, R7, R8, R9, U, V, Z, A, W, X, M, E, L, T and D are defined as in the specification, pharmaceutical compositions containing them and their use in the treatment of central nervous system and other disorders.
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Page/Page column 112-113
(2010/02/12)
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