- Synthetic Method of Intermediate for Fesoterodine
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The present invention relates to a method for producing 3-(3-diisopropylamino-1-phenylpropyl)-4-hydroxy benzenemethanol, which is an intermediate product useful for producing fesoterodine, by using ethyl benzoylacetate as a starting material. The producin
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Paragraph 0064; 0065
(2017/12/01)
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- Formal synthesis of fesoterodine by acid-facilitated aromatic alkylation
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The competitive muscarinic receptor antagonist fesoterodine is a congener of tolterodine and has better efficiency compared to tolterodine. In this study, we present an efficient synthesis of the fesoterodine intermediate 3-(3-diisopropylamino-1-phenylpropyl)-4-hydroxybenzaldehyde from ethyl benzoylacetate by Friedel-Crafts alkylation in the presence of an acid as a key reaction step. The synthesis is carried out by the reduction of the ketoester to a 1,3-diol, diisopropylamine substitution, and Friedel-Crafts alkylation, followed by reduction and chiral resolution.
- Lee, Youngeun,Shabbir, Saira,Jeong, Yuri,Ban, Jaeyoung,Rhee, Hakjune
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p. 2885 - 2889
(2016/02/05)
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- Rearrangement of ethers: A new route to tolterodine
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The rearrangement of benzyl phenolic ether in the presence of an acid or AlCl3 is utilized to produce biphenyl methane compounds in very good yields. The synthesis of muscarine receptor antagonist tolterodine is described.
- Arava, Veera Reddy,Bandatmakuru, Sreenivasula Reddy,Malreddy, Sashibhushan,Golla, Narayanaswamy
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experimental part
p. 1565 - 1571
(2011/06/27)
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- Selective nosylation of 1-phenylpropane-1,3-diol and perchloric acid mediated Friedel-Crafts alkylation: Key steps for the new and straightforward synthesis of tolterodine
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We have developed a new and straightforward synthesis of racemic tolterodine [N,N-diisopropyl-3-(2-hydroxy-5-methyl-phenyl)-3-phenylpropanamine]. The synthesis involves selective nosylation on the primary alcohol of 1-phenylpropane-1,3-diol using 4-nitrob
- De Castro, Kathlia A.,Rhee, Hakjune
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body text
p. 1841 - 1844
(2009/04/04)
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- PROCESS FOR PREPARATION OF 3-(2-HYDROXY-5-SUBSTITUTED PHENYL)-N-ALKYL-3-PHENYLPROPYLAMINES
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A new process for preparation of 3-(2-hydroxy-5-substituted phenyl)-N,alkyl-3- phenylpropylamiηes from cinamoyl chloride via N-alky-3-phenylprop-2-en-1 -amine has been developed.
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Page/Page column 10
(2008/06/13)
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