69999-16-2Relevant articles and documents
Darifenacin intermediate 2, 3 - dihydro - 5 - benzofuran acetic acid preparation new method of (by machine translation)
-
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)
SUBSTITUTED PYRROLIDINES
-
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
-
, (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.