1132832-75-7Relevant articles and documents
Preparation method of intermediate
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, (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.
Synthesis method of canagliflozin intermediate
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, (2018/03/26)
The invention relates to a synthesis method of a canagliflozin intermediate. Concretely, succinyl oxide and fluorobenzene are used as starting raw materials to be prepared into the canagliflozin crucial intermediate of 2-(4-fluorophenyl)-5-[(5-halogen-2-methyl phenyl)methyl]thiophene through the steps of Friedel-Crafts acylation ring opening, thiophene ring preparation, Friedel-Crafts acylation coupling, reduction and the like. The cheap succinyl oxide is used for preparing the thiophene ring, so that the Suzuki coupling reaction and Grignard reaction are avoided; the use of heavy metal reagents of palladium and the like is avoided; the production process is simplified; the product yield and the quality are improved; the environment pollution is reduced; the production cost is reduced.
Deuterium-modified carbon glycoside derivate
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Paragraph 0089; 0090; 0091; 0098; 0099; 0100, (2016/12/26)
The invention belongs to the field of medinal chemistry and relates to a deuterium-modified carbon glycoside derivate, in particular to a compound shown in the formula I. The invention further relates to a preparation method of the deuterium-modified carbon glycoside derivate, a medicine composition comprising the deuterium-modified carbon glycoside derivate and application of the deuterium-modified carbon glycoside derivate or the medicine composition thereof for preparing medicine for treating diabetes.