- Design, Synthesis, and Molecular Modeling of Asymmetric Tolterodine Derivatives as Anticancer Agents
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An efficient and short enantioselective synthesis of (S)- and (R)-tolterodine acid isomers (7a–7i) was performed a 6-methyl-4-phenylchroman-2-one intermediate from inexpensive and commercially available starting materials. A series of tolterodine acid hyb
- Dakarapu, Veera venkatarao,Allaka, Tejeswara Rao,Uppalla, Lav Kumar,Jha, Anjali
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p. 2157 - 2167
(2018/09/19)
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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 203-211
(2010/09/03)
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- METHOD OF OBTAINING 3,3-DIPHENYLPROPYLAMINES
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The invention relates to a method of obtaining 3,3-diphenylpropylamines (I), wherein R1 is H, alkyl, haloalkyl or alkoxyalkyl, R2 is alkyl, alkoxy, halogen, NO2, CN, CHO, which may be free or protected, CH2OH or COOR6, and R3 and R4 are selected independently from H and alkyl or together with the nitrogen to which they are bound form a ring having 3 to 7 members. The inventive method consists in reacting a propylenephenylamine and a disubstituted aromatic hydrocarbon and, if necessary, separating the desired enantiomer or the mixture of enantiomers, and/or converting the compound (I) into a salt. Compounds (I) are muscarinic receptor antagonists which can be used in the treatment of urinary incontinence and other symptoms of urinary bladder hyperactivity. Said compounds include tolterodine.
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Page/Page column 10
(2008/12/05)
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- PROCESS FOR PREPARING 3,3-DIARYLPROPYLAMINES
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Described is a process of preparing a pure solid or crystalline racemic 3,3- diarylpropylamine compound and the compounds formed thereof. The solid and crystalline forms of racemic 3,3-diarylpropylamine compound are especially suitable for producing highl
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Page/Page column 10-11
(2008/06/13)
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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 10
(2008/06/13)
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- 3,3-DIARYLPROPYLAMINE DERIVATIVES AND PROCESSES FOR ISOLATION THEREOF
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The invention relates to 3,3-diarylpropylamines derivatives and processes for producing them. More particularly, it relates to the preparation of pure tolterodine or a pharmaceutically acceptable salt thereof and pharmaceutical compositions that include t
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