69999-16-2Relevant academic research and scientific papers
Darifenacin intermediate 2, 3 - dihydro - 5 - benzofuran acetic acid preparation new method of (by machine translation)
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Paragraph 0060; 0061; 0062, (2018/04/03)
The invention relates to a darifenacin intermediate - 2, 3 - dihydro - 5 - benzofuran acetic acid. By the P-hydroxy-acetic acid and bromo acetaldehyde acetal as the starting material, the presence of O - alkylation reaction under a condition of the corresponding ether compound; then by esterification reaction to obtain the corresponding ester; in PPA (poly phosphoric acid) under the action of the, cyclization to obtain 2, 3 - benzofuran - 5 - acetate; 2, 3 - benzofuran - 5 - acetic acid layer which hydrolysis, to acidify the corresponding carboxylic acid; obtained by catalytic hydrogenation of 2, 3 - dihydro - 5 - benzofuran acetic acid; or the first 2, 3 - benzofuran - 5 - acetate obtained by catalytic hydrogenation of 2, 3 - dihydro - 5 - benzofuran acetic acid esters; and hydrolyzed, acidified to obtain 2, 3 - dihydro - 5 - benzofuran acetic acid. The method of the invention by simple and safe, each reaction raw materials are cheap and easy to obtain, the reaction yield is high, and is particularly suitable for industrial production of 2, 3 - dihydro - 5 - benzofuran acetic acid. (by machine translation)
Novel preparation method of darifenacin intermediate 2,3-dihydro-5-benzofuran acetic acid
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Paragraph 0047; 0048; 0049, (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.
HIV-1 VIRION MATURATION INHIBITORS, COMPOSITIONS AND TREATMENTS USING THE SAME
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Page/Page column 30-31, (2008/06/13)
The present invention provides compounds of Formula I, II, III or IV, or pharmaceutically acceptable salts and solvates thereof, which are useful as inhibitors of human immunodeficiency virus (HIV) and are also useful for the treatment of HIV infections in HIV- infected mammals, including humans. The present invention also provides pharmaceutical compositions comprising compounds of Formula I1 II, III or IV, and their pharmaceutically acceptable salts and solvates.
(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.
