1030825-20-7Relevant articles and documents
METHOD FOR PRODUCING 5-BROMO-2-ALKYLBENZOIC ACID
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Paragraph 0068; 0072-0074, (2021/09/03)
PROBLEM TO BE SOLVED: To provide a method for producing 5-bromo-2-alkylbenzoic acid, which is useful as a synthetic intermediate of a drug substance such as an antidiabetic, in an industrially inexpensive and efficient manner. SOLUTION: The present disclosure provides a method for producing 5-bromo-2-alkylbenzoic acid by bringing 2-alkylbenzoic acid and bromine into contact with each other, in the presence of sulfuric acid. Particularly if 2-alkylbenzoic acid is 2-methylbenzoic acid, the inventive production method enables efficient production of 5-bromo-2-methylbenzoic acid to be a raw material for producing canagliflozin, one of antidiabetics. SELECTED DRAWING: None COPYRIGHT: (C)2021,JPOandINPIT
Preparation method of 2-(4-fluorophenyl)-5-[(5-bromo-2-methylphenyl)methyl]thiophene
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, (2020/04/17)
The invention belongs to the field of chemistry, and particularly relates to a novel synthesis method of a key intermediate 2-(4-fluorophenyl)-5-[(5-bromo-2-methylphenyl)methyl]thiophene for preparinga medicine canagliflozin for treating type 2 diabetes mellitus. Cheap and easily available 2-methylthiophene used as an initial raw material undergoes five steps of halogenation, p-nitrotoluene alkylation, coupling, nitro reduction and a Sandmeyer reaction to prepare the product. The method has the characteristics of simplicity in operation, high reaction selectivity, few byproducts and high product quality.
Preparation method for canagliflozin intermediate
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, (2020/03/09)
The invention relates to a preparation method for a canagliflozin intermediate. The canagliflozin key intermediate, namely 2-(4-fluorophenyl)-5-[(5-bromo-2-methylphenyl)methyl]thiophene is obtained through a three-step reaction of coupling, N-halogenated succinimide halogenation and p-bromotoluene alkylation by using easily-available 2-bromo-5-methylthiophene as a starting raw material. The preparation method provided by the invention has the characteristics of easily-available raw materials, short production steps, simple operation, stable process, high yield and good product quality.