133034-00-1Relevant articles and documents
Correction to: Rhodium/yanphos-catalyzed asymmetric interrupted intramolecular hydroaminomethylation of trans-1,2-disubstituted alkenes (J. Am. Chem. Soc. (2016) 138 (9017?9020) (DOI: 10.1021/jacs.6b03596)
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supporting information, p. 4230 - 4230 (2017/03/30)
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IMPROVED PROCESS FOR PRODUCING DARIFENACIN
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Page/Page column 7; 9, (2009/11/29)
The present invention discloses an improved process for producing darifenacin, the process comprising decarboxylating (2S,4R)-4-hydroxy-2-pyrrolidine carboxylic acid followed by in situ tosylation to give l-tosyl-3-(R)-(-)-hydroxypyrrolidine, tosylating the l-tosyl-3-(R)-(-)-hydroxypyrrolidine with methyl-p-toluenesuolphonate to give l-tosyl-3- (S)-(-)-tosyloxy pyrrolidine, reacting l-tosyl-3-(S)-(-)-tosyloxy pyrrolidine with diphenyl acetonitrile in presence of a base to give 3-(S)-(+)-(l-cyano-l,l-diphenylmethyl)-l- tosylpyrrolidine, de-protecting 3-(S)-(+)-(l-cyano-l,l-diphenylmethyl)-l- tosylpyrrolidine in the presence of phenol in acidic medium to give 3-(S)-(+)-(l-cyano- 1,1-diphenylmethyl) pyrrolidine, hydrolyzing 3-(S)-(+)-(l-cyano-l,l-diphenylmethyl) pyrrolidine followed by salt formation to obtain 3-(S)-(+)-(l-carbamoyl-l,l- diphenylmethyl)pyrrolidine.L-(+)-tartrate, condensing 3-(S)-(+)-( 1 -carbamoyl- 1,1- diphenylmethyl)pyrrolidine-L(+)-tartrate with 5-(2-bromoethyl)-2,3-dihydrobenzofuran employing a base in a solvent to give darifenacin.
Muscarinic receptor antagonists
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, (2008/06/13)
Muscarinic receptor antagonists of formula (I), and their pharmaceutically acceptable salts, wherein Y is --CH 2 --, --(CH 2) 2 --, --CH 2 O--, --(CH 2) 2 O-- or --CH 2 S--; R is --CH or --CONH 2 ; and R 1 is a group of formula (a), where R 2 and R 3 are each independently H, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, --(CH 2) n OH, halo, trifluoromethyl, cyano, --(CH 2) n NR 4 R 5, --CO(C 1 -C 4 alkyl), --OCO(C 1 -C 4 alkyl), --CH(OH)(C 1 -C 4 alkyl), --C(OH)(C 1 -C 4 alkyl 2, --SO 2 NH 2, --(CH 2) n CONR 6 R 7 or --(CH 2) n COO(C 1 -C 4 alkyl); R 4 is H or C 1 -C 4 alkyl; R 5 is H, C 1 -C 4 alkyl or C 1 -C 4 alkysulphonyl; R 6 and R 7 are each independently H or C 1 -C 4 alkyl; and n is 0, 1 or 2. The compounds are particularly useful in treating irritable bowel syndrome.