cas 173334-58-2, Aliskiren hemifumarate | Articles data

Articles about 173334-58-2Total 15 be found

Convergent Synthesis of the Renin Inhibitor Aliskiren Based on C5-C6 Disconnection and CO2H-NH2 Equivalence
A novel synthesis of the renin inhibitor aliskiren based on an unprecedented disconnection between C5 and C6 was developed, in which the C5 carbon acts as a nucleophile and the amino group is introduced by a Curtius rearrangement, which follows a simultaneous stereocontrolled generation of the C4 and C5 stereogenic centers by an asymmetric hydrogenation. Operational simplicity, step economy, and a good overall yield makes this synthesis amenable to manufacture on scale.
Cini, Elena,Banfi, Luca,Barreca, Giuseppe,Carcone, Luca,Malpezzi, Luciana,Manetti, Fabrizio,Marras, Giovanni,Rasparini, Marcello,Riva, Renata,Roseblade, Stephen,Russo, Adele,Taddei, Maurizio,Vitale, Romina,Zanotti-Gerosa, Antonio
p. 270 - 283
(2016/03/04)

A new crystalline forms of lueck logical sequence half fumaric acid salt and its preparation and use
The invention relates to a new crystal form of Aliskiren hemifumarate. The X-ray powder diffraction pattern of the new crystal form of Aliskiren hemifumarate has absorption peaks when 2theta is at 7.0(+/-0.30)DEG, 8.6(+/-0.30)DEG and 10.0(+/-0.30)DEG. The invention also relates to a preparation method of the new crystal form of Aliskiren hemifumarate through a low alcohol re-crystallization process. The new crystal form of Aliskiren hemifumarate has the characteristics of good fluidity and easy granulation.
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Paragraph 0032; 0033

(2017/04/04)

Chemical process for opening ring compounds
It is described a process for the opening of lactone or lactam rings useful in the synthesis of pharmaceutically active compounds and the intermediates thereof, particularly Aliskiren. It has found that by selecting a type of solvent it is possible to obtain excellent yields and high optical and chemical purity of the isolated products.
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Paragraph 0101; 0102; 0103; 0104; 0105

(2013/03/26)

CHEMICAL PROCESS FOR OPENING RING COMPOUNDS
It is described a process for the opening of lactone or lactam rings useful in the synthesis of pharmaceutically active compounds and the intermediates thereof, particularly Aliskiren. It has found that by selecting a type of solvent it is possible to obtain excellent yields and high optical and chemical purity of the isolated products.
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Page/Page column 19

(2013/03/26)

PROCESS FOR THE PREPARATION OF ALISKIREN
The present invention relates to an improved process for the preparation of Aliskiren and its pharmaceutically acceptable salts comprising reducing the compound of Formula-Z in presence of catalyst and ammonia. The present invention further relates to Aliskiren hemifumarate having diastereomeric impurity less than 0.2%.(F) H3C CH3 NH2 H3C 0 H3C CH3 Formula-Z
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(2013/10/21)

End-to-end continuous manufacturing of pharmaceuticals: Integrated synthesis, purification, and final dosage formation
A series of tubes: The continuous manufacture of a finished drug product starting from chemical intermediates is reported. The continuous pilot-scale plant used a novel route that incorporated many advantages of continuous-flow processes to produce active pharmaceutical ingredients and the drug product in one integrated system. Copyright
Mascia, Salvatore,Heider, Patrick L.,Zhang, Haitao,Lakerveld, Richard,Benyahia, Brahim,Barton, Paul I.,Braatz, Richard D.,Cooney, Charles L.,Evans, James M. B.,Jamison, Timothy F.,Jensen, Klavs F.,Myerson, Allan S.,Trout, Bernhardt L.
p. 12359 - 12363
(2013/12/04)

PROCESS FOR THE PREPARATION OF ALISKIREN
The present invention provides a novel process and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren, or a salt thereof, preferably Aliskiren hemifumarate.
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Page/Page column 25

(2013/05/21)

SYNTHESIS OF ALISKIREN
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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(2012/05/05)

ALISKIREN INTERMEDIATES AND A PROCESS FOR ANALYZING THE PURITY OF ALISKIREN
The present invention provides aliskiren intermediates and impurities, and processes for preparation thereof. The present invention also provides processes for preparing aliskiren using these intermediates and impurities. These impurities can also be used as reference markers or reference standards in the determination of the purity of aliskiren or intermediates of aliskiren.
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Page/Page column 24

(2012/03/27)

PROCESS FOR THE PREPARATION OF (2S,4S,5S,7S)-N-(2-CARBAMYL-2- METHYLPROPYL)-5-AMINO-4-HYDROXY-2,7-DIISOPROPYL-8-[4-METHOXY-3-(3- METHOXYPROPOXY)PHENYL]-OCTANAMIDE HEMIFUMARATE AND ITS INTERMEDIATES THEREOF
The present invention relates to a process for the preparation of (2S,4S,5S,7S)-N-(2- Carbamoyl-2-methylpropyl)-5-amino-4-hydroxy-2,7-diisopropyl-8-[4-methoxy-3-(3-methoxy propoxy )phenyl]-octanamide compound of formula- 1 and its pharmaceutically acceptable salts thereof. Further, relates to the processes for the preparation of (R)-4-(2-(halomethyl)-3- methylbutyl)-l-methoxy-2-(3-methoxypropoxy) benzene and (R)-2-(4-methoxy-3-(3-methoxy propoxy) benzyl)-3-methyIbutan-l-ol useful intermediates in the synthesis of compound of formula- 1.
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(2011/12/14)

SYNTHESIS ROUTES TO 2(S),4(S),5(S),7(S)-2,7-DIALKYL-4-HYDROXY-5-AMINO-8-ARYL-OCTANOYL AMIDES
The invention relates to a process for the preparation of compounds that are important building blocks in convergent synthesis routes to 2(S),4(S),5(S),7(S)-2,7-dialkyl-4-hydroxy-5-amino-8-aryl-octanoyl amides or pharmaceutically acceptable salts thereof, such as the compound Aliskiren, and to a process for the preparation of these octanoyl amides, comprising reacting said building block.
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Page/Page column 50

(2010/04/03)

Process and intermediates for the preparation of aliskiren
The present invention relates to a process and intermediates for the manufacture of aliskiren or pharmaceutically acceptable salts thereof.
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Page/Page column 21; 22

(2010/06/15)

POLYMORPHIC FORMS OF ALISKIREN HEMIFUMARATE AND PROCESS FOR PREPARATION THEREOF
Provided are amorphous and polymorphic forms of aliskiren hemifumarate, pharmaceutical compositions thereof, and processes for their preparation.
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Page/Page column 19

(2009/06/27)

Process and intermediates for the preparation of aliskiren
The present invention relates to a process and intermediates for the manufacture of aliskiren or pharmaceutically acceptable salts thereof.
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Page/Page column 15-16

(2009/06/27)

METHODS OF TREATING ALZHEIMER'S DISEASE USING ARYL ALKANOIC ACID AMIDES
Disclosed are methods for treating Alzheimer’s disease, and other diseases, and/or inhibiting beta-secretase enzyme, and/or inhibiting deposition of A beta peptide in a mammal, by use of compounds of formula 1 (1) wherein the variables R1-R8 and X are defined herein.
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Page 196

(2010/02/05)