411221-53-9Relevant academic research and scientific papers
Preparation method of citalopram impurities
-
Paragraph 0025; 0034-0035; 0038, (2021/03/31)
The invention relates to a preparation method of a citalopram impurity. The preparation method comprises the following steps: oxidizing free 4-[4-(dimethylamino)-1-(4-fluorophenyl)-1-hydroxybutyl]-3-hydroxybutyl]-3-hydroxymethyl benzonitrile hydrobromide and a Jones reagent to prepare a citalopram impurity C; and carrying out a reduction reaction with DIBAL-H by using the citalopram impurity C asa raw material to prepare a citalopram impurity B, wherein the citalopram impurity B is 1-(3-(dimethylamino)propyl)-1-(4-fluorophenyl)-3-hydroxy-1,3-dihydro-5-nitrile isobenzofuran. According to the invention, the citalopram impurity can be stably obtained at high yield, so that a basis is provided for qualitative and quantitative determination of the impurity in a raw material medicine synthesisprocess.
CHEMOSELECTIVE METHYLENE HYDROXYLATION IN AROMATIC MOLECULES
-
Paragraph 0230; 0472-0474, (2020/03/28)
A chemoselective and reactive Mn(CF3-PDP) catalyst system that enables for the first time the strategic advantages of late-stage aliphatic C—H hydroxylation to be leveraged in aromatic compounds. This discovery will benefit small molecule therapeutics by enabling the rapid diversification of aromatic drugs and natural products and identification of their metabolites.
Chemoselective methylene oxidation in aromatic molecules
Zhao, Jinpeng,Nanjo, Takeshi,de Lucca, Emilio C.,White, M. Christina
, p. 213 - 221 (2019/01/04)
Despite significant progress in the development of site-selective aliphatic C–H oxidations over the past decade, the ability to oxidize strong methylene C–H bonds in the presence of more oxidatively labile aromatic functionalities remains a major unsolved
Synthesis method of aryl alcohol compound and Escitalopram
-
Paragraph 0151 - 0153, (2016/10/10)
The invention discloses a synthesis method of an aryl alcohol compound and Escitalopram. The synthesis method of the aryl alcohol compound comprises the following steps: under gas protection and in an organic solvent and in the presence of transition metal, diphosphine ligand and alkali, the compound of formula 1 reacts with an aryl boron reagent 2. The synthesis method of Escitalopram comprises the following steps: (1) under gas protection and in an organic solvent and in the presence of transition metal, diphosphine ligand and alkali, the compound of formula 4 reacts with the aryl boron reagent 2; (2) under gas protection and in an organic solvent and in the presence of alkali, the compound of formula 5 reacts with dimethylamine or hydrochloride thereof; (3) under gas protection and in an organic solvent and in the presence of organic phosphine ligand and a palladium catalyst, the compound of formula 7 reacts with metal cyanide; and (4) under gas protection and in an organic solvent and in the presence of a reducing agent, the compound of formula 6 reacts. The synthesis method disclosed by the invention has high yield and enantioselectivity.
