461432-25-7Relevant articles and documents
Copper-Catalyzed Arylation of Benzylic C-H bonds with Alkylarenes as the Limiting Reagents
Zhang, Wen,Chen, Pinhong,Liu, Guosheng
, p. 7709 - 7712 (2017)
A novel copper-catalyzed arylation of benzylic C-H bonds with nucleophilic arylboronic acids has been developed that provides an efficient way to synthesize various 1,1-diarylalkanes with a broad substrate scope and excellent functional group compatibilit
Preparation method of dapagliflozin
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, (2020/05/05)
The invention relates to a preparation method of dapagliflozin. The preparation method comprises the following steps: by using 1-chloro-2-(4-ethoxybenzyl)-4-iodobenzene as an initial raw material, reacting with magnesium by using iodine granules as an initiator to prepare a Grignard reagent of iodo-benzene; carrying out bromination reaction on peracetylated sugar and hydrogen bromide in an aceticacid solution to prepare 2,3,4,6-tetraacetylglucosamine bromide; adding the prepared Grignard reagent of iodo-benzene into a methylbenzene/tetrahydrofuran solution, dropwise adding a rare earth catalyst and 2,3,4,6-tetraacetylglucosamine bromide into the methylbenzene/tetrahydrofuran solution, reacting to obtain an intermediate compound of dapagliflozin; and adding the prepared intermediate compound of dapagliflozin into a tetrahydrofuran/ethanol/water solution of sodium hydroxide, removing acetyl after alkaline hydrolysis, and re-crystallizing to obtain dapagliflozin. The reaction raw materials are easy to obtain, the preparation method is simple, the conditions are mild, the preparation method is safer and more environmentally friendly, the yield is high, the purity can reach 99%, and the method is suitable for large-scale production.
Carbon-aryl glycoside SGLT-2 inhibitor precursor and synthesis method thereof
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Paragraph 0026, (2019/03/28)
The invention relates to a plurality of carbon-aryl glycoside SGLT-2 inhibitor precursors and a synthesis method thereof. The method takes glycosyl bromide and aryl iodide (bromide) as substrates, thesubstrates react for 1-2 days through ice water bath and the room temperature mixing condition under the effects of a catalyst, a ligand, a reducing agent and an additive, and a precursor compound ofcarbon-aryl glycoside SGLT-2 inhibitor drug is obtained. The synthesis method has the advantages that the precursor compound is convenient to hydrolyze, the conversion rate is high, the catalyst metal is cheap, the product is easily and massively prepared and not prone to deteriorating, the reaction is moderate, one-pot reaction and one-step reaction are achieved, the steps are simple, the methodis safe to operate, the yield is high, and the stereoscopic selectivity is good.