79002-49-6Relevant academic research and scientific papers
Novel preparation method of darifenacin intermediate 2,3-dihydro-5-benzofuran acetic acid
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Paragraph 0038; 0039; 0040, (2018/04/03)
The invention relates to a novel preparation method of a darifenacin intermediate 2,3-dihydro-5-benzofuran acetic acid. The method comprises the following steps: by taking 2,3-dihydrobenzofuran as aninitial raw material in the presence of a Lewis acid, carrying out a Friedel-Crafts acylation reaction with ethyl oxalyl monochloride so as to obtain a corresponding acyl compound; hydrolyzing to obtain alpha-ketonic acid sodium salt; reducing carbonyl into methylene by utilizing a Wolff-Kishner-HuangMinlong reaction, and acidizing, thereby obtaining the 2,3-dihydro-5-benzofuran acetic acid. The method disclosed by the invention is simple, convenient and safe, cheap and readily available in reactive raw materials and high in reaction yield and is particularly suitable for industrialized production of the 2,3-dihydro-5-benzofuran acetic acid.
Acylation of aromatic ethers over solid acid catalysts: Scope of the reaction with more complex acylating agents
Smith, Keith,El-Hiti, Gamal A.,Jayne, Anthony J.,Butters, Michael
, p. 2321 - 2325 (2007/10/03)
Acylation of anisole with 2-phenylbutanoic acid derivatives, over zeolite catalysts, gives the corresponding 4-acyl derivatives with high regioselectivity. In an analogous way, 2,3-dihydrobenzofuran reacts with acid anhydrides or chlorides in the presence
Heterobicyclic keto- and amino-acids, esters and amides
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, (2008/06/13)
Heterobicyclic glyoxylic acids, L- and DL-heterobicyclic glycines and their derivatives of the formulae STR1 and pharmaceutically acceptable cationic and acid addition salts thereof, wherein R is OR2 or NHR3 ; R2 is hydrogen or alkyl having from one to four carbon atoms; R3 is hydrogen, alkyl having from one to four carbon atoms, alkoxyalkyl having from one to four carbon atoms in each of the alkyl groups or R4 R5 C6 H3 CH2 -- where R4 and R5 are H, OH, F, Cl, Br, I, or alkyl or alkoxy having from one to four carbon atoms R1 is hydrogen, alkyl having from one to four carbon atoms or R4 R5 C6 H3 --; X is oxygen or sulfur; n is 0 or 1 and the broken line represents an optionally present double bond; useful in treatment of diseases and conditions which are characterized by reduced blood flow, reduced oxygen availability or reduced carbohydrate metabolism in the cardiovascular system.
