- A aliskiren or its salt separation and analysis method
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The invention relates to a separation analysis method using polysaccharide derivative-bonded and coated silica as a stationary phase and an organic solvent as a mobile phase for separation analysis of aliskiren and isomers thereof, effective separation of the aliskiren and isomers thereof can be realized, and the separation analysis method has the important meaning to the product quality control.
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- SYNTHESIS OF ALISKIREN
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The present invention provides novel process for the preparation of renin inhibitor Aliskiren or its derivatives, and its pharmaceutically acceptable salts. The present invention also provides novel intermediates used in the preparation of Aliskiren.
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- A total synthesis of aliskiren
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A total synthesis of aliskiren (20) was accomplished. A key in our synthesis was to use the symmetric trans-cisoid-trans-bis-lactone 1 as a precursor. It was expediently prepared by three different routes (Scheme 2). Appending the end groups and functional group transformations completed the synthesis (Scheme 3). Copyright
- Nam, Gyeok,Ko, Soo Y.
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p. 1937 - 1945,9
(2012/12/12)
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- AMIDE INHIBITORS OF RENIN
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The present invention relates to new amide inhibitors of renin, pharmaceutical compositions thereof, and methods of use thereof
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- PROCESS FOR THE PREPARATION OF SUBSTITUTED OCTANOYL AMIDES
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Compounds of formula (XII), are simultaneously halogenated in the 5 position and hydroxylated in the 4 position under lactonization, the halolactone is reacted with an amine to form a carboxamide, the halogen is replaced with azide, if necessary after the introduction of a hydroxy protecting group, the resulting azide is converted to a lactone, the lactone is amidated and then the azide converted to the amine group, in order to obtain compounds of formula (I) or a salt thereof.
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- A convergent synthesis approach towards CGP60536B, a non-peptide orally potent renin inhibitor, via an enantiomerically pure ketolactone intermediate
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We report a convergent synthesis of the potent orally active non-peptide renin inhibitor CGP60536B. The key reaction employs the coupling of the enantiopure Grignard species derived from chloride 13 with the diastereomerically pure γlactone 9b. The stereoselective reduction of the resulting ketone 14b has been thoroughly investigated. (C) 2000 Elsevier Science Ltd.
- Rueger,Stutz,Goschke,Spindler,Maibaum
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p. 10085 - 10089
(2007/10/03)
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- A convergent synthesis of the renin inhibitor CGP60536B
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Pseudoephedrine serves as a dual purpose chiral auxiliary and protecting group in the synthesis of the novel orally active renin inhibitor CGP60536B. (C) 2000 Elsevier Science Ltd.
- Sandham,Taylor,Carey,Fassler
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p. 10091 - 10094
(2007/10/03)
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