1030825-20-7Relevant articles and documents
METHOD FOR PRODUCING 5-BROMO-2-ALKYLBENZOIC ACID
-
Paragraph 0068; 0075-0078, (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 intermediate
-
Paragraph 0025; 0029, (2020/06/29)
The invention discloses a preparation method for a Canagliflozin intermediate. The preparation method comprises the steps that substituted bromobenzene as a starting material is reacted with bisdiboron to prepare a boride, and then the Canagliflozin intermediate is prepared through a Suzuki coupling reaction, a Friedel-Crafts acylation reaction and a reduction reaction. The preparation method hasthe advantages that the intermediate product CZ-2 is prepared through the Suzuki coupling reaction, the conditions are mild and easy to operate and control, and the product yield and the product purity are high; aryl methyl is introduced through the Friedel-Crafts acylation reaction, a main chain is built, by means of the route, the yield is high, technological conditions are easy to control, andthe preparation method is suitable for large-scale industrial production.
Preparation method for canagliflozin intermediate
-
, (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.