- Iron-catalyzed regioselective transfer hydrogenative couplings of unactivated aldehydes with simple alkenes
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An FeBr3-catalyzed reductive coupling of various aldehydes with alkenes that proceeds through a direct hydride transfer pathway has been developed. With iPrOH as the hydrogen donor under mild conditions, previously challenging coupling reactions of unactivated alkyl and aryl aldehydes with simple alkenes, such as styrene derivatives and α-olefins, proceeded smoothly to furnish a diverse range of functionalized alcohols with complete linear regioselectivity. The reductive coupling of various aldehydes and alkenes through a direct hydride transfer pathway can be catalyzed by FeBr3. With isopropanol as the hydrogen donor, previously challenging coupling reactions of unactivated alkyl and aryl aldehydes with simple alkenes, such as styrene derivatives and α-olefins, proceeded smoothly to furnish a diverse range of functionalized alcohols with complete linear regioselectivity.
- Zheng, Yan-Long,Liu, Yan-Yao,Wu, Yi-Mei,Wang, Yin-Xia,Lin, Yu-Tong,Ye, Mengchun
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supporting information
p. 6315 - 6318
(2016/05/24)
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- Chiral Diarylmethanes via Copper-Catalyzed Asymmetric Allylic Arylation with Organolithium Compounds
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A highly enantioselective copper/N-heterocyclic carbene catalyzed allylic arylation with organolithium compounds is presented. The use of commercial or readily prepared aryllithium reagents in the reaction with allyl bromides affords a variety of chiral diarylvinylmethanes, comprising a privileged structural motif in pharmaceuticals, in high yields with good to excellent regio- and enantioselectivities. The versatility of this new transformation is illustrated in the formal synthesis of the marketed drug tolterodine (Detrol).
- Guduguntla, Sureshbabu,Hornillos, Valentín,Tessier, Romain,Fa?anás-Mastral, Martín,Feringa, Ben L.
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p. 252 - 255
(2016/02/03)
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- PROCESS FOR THE PREPARATION OF (R)-2-(3-DIISOPROPYLAMINO)-1-PHENYLPROPYL)-4METHYLPHENOL AND SALTS THEREOF
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The present invention relates to an improved process for the preparation of Tolterodine or salts thereof, which comprises the use of 3-(2-methoxy-5-methylphenyl)-3-phenylpropyl methane sulfonate.
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Page/Page column 4
(2012/03/08)
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- A PROCESS FOR THE PREPARATION OF TOLTERODINE TARTRATE
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The present invention relates to provide an improved process for the preparation of tolterodine or salt thereof, comprises a step of reducing 3-(2-methoxy-5-methylphenyl) -3-phenyl propionic acid of formula (III) in the presence of a reducing agent, an acidic reagent and a solvent to obtain 3-(2-methoxy-5-methylphenyl) -3-phenyl propanol of formula (IV).
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Page/Page column 16
(2010/05/13)
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- A PROCESS FOR THE PREPARATION OF TOLTERODINE TARTRATE
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The present invention relates to provide a process for the preparation of (+)-(R)-Tolterodine-L-tartrate, comprises a step of aminating hydroxyl protected 3-(2-methoxy-5-methylphenyl)-3-phenyl propanol of formula (V) with diisopropylamine in the presence of water to obtain N, N-diisopropyl-3-(2-methoxy-5-methylphenyl)-3-phenylpropyl amine of formula (VI).
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Paragraph 157-164
(2010/09/03)
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- IMPROVED PROCESS FOR THE PREPARATION OF (R)-2-(3-DIISOPROPYLAMINO)-1-PHENYLPROPYL)-4METHYLPHENOL AND SALTS THEREOF
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The present invention relates to an improved process for the preparation of Tolterodine or salts thereof, which comprises the use of 3-(2-methoxy-5-methylphenyl)-3-phenylpropyl methane sulfonate.
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Page/Page column 6
(2010/09/17)
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- Process for the preparation of tolterodine
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A novel process for the preparation of tolterodine, i.e. (R)-N,N-diisopropyl-3-(2-hydroxy-5-methylphenyl)-3-phenylpropanamine, in the racemic form, as well as intermediates useful for its preparation.
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Page/Page column 5-6
(2008/06/13)
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- A process for the preparation of tolterodine
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A novel process for the preparation of tolterodine (I), i.e. (R)-N,N-diisopropyI-3-(2-hydroxy-5-methylphenyl)-3-phenylpropanamine, in the racemic form, as well as intermediates useful for its preparation.
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Page/Page column 8-9
(2010/11/23)
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- METHOD OF OBTAINING TOLTERODINE
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The process comprises reacting a compound of formula (II), where R is a hydroxyl protecting group, and the asterisk indicates an asymmetric carbon atom, with diisopropylamine in the presence of a reducing agent; optionally converting the resulting intermediate into a salt and, if so desired, isolating it; removing the hydroxyl protecting group; and if so desired, separating the desired (R) or (S) enantiomer, or the mixture of enantiomers and/or converting the obtained compound into a pharmaceutically acceptable salt thereof. Tolterodine is a muscarinic receptor antagonist useful in treating urinary incontinence and other symptoms of urinary bladder hyperactivity.
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Page/Page column 9
(2008/06/13)
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- TOLTERODINE, COMPOSITIONS AND USES THEREOF, AND PREPARATION OF THE SAME
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Racemic tolterodine free base in crystalline form, tolterodine with improved purity, compositions and uses thereof, and processes of preparing the same.
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Page/Page column 12-13
(2008/06/13)
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- 3,3-DIPHENYLPROPYLAMINES AND PHARMACEUTICAL COMPOSITIONS THEREOF
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Novel 3,3-diphenylpropylamines of formula (I) wherein R1 signifies hydrogen or methyl, R2, R3 and R4 independently signify hydrogen, methyl, methoxy, hydroxy, carbamoyl, sulphanoyl or halogen, and X represents a tertiary amino group -NR5, R6, wherein R5 and R6 signify non-aromatic hydrocarbyl groups, which may be the same or different and which together contain at least three carbon atoms, and which may form a ring together with the amine nitrogen, their salts with physiologically acceptable acids and, when the compounds can be in the form of optical isomers, the racemic mixture and the individual enantiomers, their use as drugs, especially as anticholinergic agents, their use for preparing an anticholinergic drug, pharmaceutical compositions containing the novel amines, and methods for preparing the same
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