69999-16-2Relevant articles and documents
Novel preparation method of darifenacin intermediate 2,3-dihydro-5-benzofuran acetic acid
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, (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.
SUBSTITUTED PYRROLIDINES
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Page/Page column 31, (2009/01/24)
Disclosed herein are substituted pyrrolidine-based muscarinic receptor modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
(2,3-dihydro-5-benzofuranyl)-acetonitrile
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, (2008/06/13)
The novel compound (2,3-dihydro-5-benzofuranyl)-acetonitrile is prepared by chloromethylating 2,3-dihydro-benzofuran and reacting the resulting 2,3-dihydro-5-chloromethyl-benzofuran with a cyanide. (2,3-Dihydro-5-benzofuranyl)-acetonitrile can be converted by saponification to (2,3-dihydro-5-benzofuranyl)-acetic acid, an important intermediate for the manufacture of various pharmaceutical active substances. This intermediate has hitherto been obtainable only by a laborious procedure and in low yields.