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856676-23-8

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856676-23-8 Usage

Description

Choline fenofibrate, a salt formulation of fenofibric acid, is a lipid regulating agent available as delayed release capsules for oral administration. It is indicated in combination with a statin to reduce TG and increase high-density lipoprotein cholesterol (HDL-C) in patients with mixed dyslipidemia and coronary heart disease (CHD) or a CHD-risk equivalent who are optimal for statin therapy to achieve their lowdensity lipoprotein cholesterol (LDL-C) goal. In addition, choline fenofibrate is indicated as monotherapy in patients with severe hypertriglyceridemia to reduce TG, and in patients with primary hyperlipidemia or mixed dyslipidemia to reduce elevated LDL-C, total cholesterol, TG, apolipoprotein B, and to increase HDL-C. Fenofibric acid is also the active metabolite of fenofibrate (Tricor), which has been previously marketed for the treatment of hypercholesterolemia and hypertriglyceridemia. The primary mode of action of fenofibric acid is through the activation of the nuclear transcription factor PPARa, predominantly expressed in tissues that metabolize fatty acids, such as the liver, kidney, heart, and muscle.On activation by binding of the fibrate, PPARa binds as heterodimers with retinoid X receptor (RXR), which subsequently recognizes and binds to specific PPARa-response elements leading to modulation of expression of the target genes. In particular, the activity of lipoprotein lipase is increased and synthesis of apoprotein C-III is decreased, which together enhance the clearance of circulating TG-rich lipoproteins. The resulting fall in TG produces an alteration in the size and composition of LDL from small dense particles to large buoyant particles. These larger particles have a greater affinity for cholesterol receptors and are catabolized rapidly. Choline fenofibriate acid is contraindicated in patients with severe renal impairment.

Chemical Properties

White Solid

Originator

Abbott (United States)

Uses

Different sources of media describe the Uses of 856676-23-8 differently. You can refer to the following data:
1. A new formulation of fenofibric acid, ABT-335, co-administered with statins.
2. A new formulation of fenofibric acid, ABT-335,

Brand name

TriLipix

Side effects

The most common adverse reactions observed with the use of fenofibric acid alone or in combination with a statin are headache, back pain, nasopharyngitis, nausea, myalgia, diarrhea, and upper respiratory tract infection.

Synthesis

Choline To Market, To Market 2008 enofibrate is chemically derived from p-anisole in four steps through Friedel Crafts acylation with p-chlorobenzoyl chloride to the corresponding benzophenone derivative, followed by methyl ether cleavage with hydrogen bromide, alkylation of the phenolic hydroxyl group with 2-bromo-2-methylpropanoic acid using sodium hydroxide, and finally salt formation with choline.

Check Digit Verification of cas no

The CAS Registry Mumber 856676-23-8 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 8,5,6,6,7 and 6 respectively; the second part has 2 digits, 2 and 3 respectively.
Calculate Digit Verification of CAS Registry Number 856676-23:
(8*8)+(7*5)+(6*6)+(5*6)+(4*7)+(3*6)+(2*2)+(1*3)=218
218 % 10 = 8
So 856676-23-8 is a valid CAS Registry Number.
InChI:InChI=1/C17H15ClO4.C5H14NO/c1-17(2,16(20)21)22-14-9-5-12(6-10-14)15(19)11-3-7-13(18)8-4-11;1-6(2,3)4-5-7/h3-10H,1-2H3,(H,20,21);7H,4-5H2,1-3H3/q;+1/p-1

856676-23-8SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 19, 2017

Revision Date: Aug 19, 2017

1.Identification

1.1 GHS Product identifier

Product name 2-[4-(4-chlorobenzoyl)phenoxy]-2-methylpropanoate,2-hydroxyethyl(trimethyl)azanium

1.2 Other means of identification

Product number -
Other names Choline fenofibrate

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:856676-23-8 SDS

856676-23-8Synthetic route

fenofibrate
49562-28-9

fenofibrate

cholin hydroxide
123-41-1

cholin hydroxide

choline fenofibrate
856676-23-8

choline fenofibrate

Conditions
ConditionsYield
In ethanol at 80℃; for 5h; Solvent; Large scale;100%
fenofibric acid
42017-89-0

fenofibric acid

choline chloride
67-48-1

choline chloride

choline fenofibrate
856676-23-8

choline fenofibrate

Conditions
ConditionsYield
Stage #1: fenofibric acid With triethylamine In ethanol
Stage #2: choline chloride In ethanol Reflux;
75%
Stage #1: fenofibric acid With triethylamine In ethanol for 10 - 15h;
Stage #2: choline chloride In ethanol Reflux;
75%
ethyl 2-bromoisobutyrate
600-00-0

ethyl 2-bromoisobutyrate

4-chloro-4'-hydroxybenzophenone
42019-78-3

4-chloro-4'-hydroxybenzophenone

cholin hydroxide
123-41-1

cholin hydroxide

choline fenofibrate
856676-23-8

choline fenofibrate

Conditions
ConditionsYield
Stage #1: ethyl 2-bromoisobutyrate; 4-chloro-4'-hydroxybenzophenone With potassium carbonate at 145℃; for 3h;
Stage #2: cholin hydroxide In propan-1-ol; water for 3h; Heating / reflux;
70%
isopropyl 2-bromo-2‑methylpropanoate
51368-55-9

isopropyl 2-bromo-2‑methylpropanoate

4-chloro-4'-hydroxybenzophenone
42019-78-3

4-chloro-4'-hydroxybenzophenone

cholin hydroxide
123-41-1

cholin hydroxide

choline fenofibrate
856676-23-8

choline fenofibrate

Conditions
ConditionsYield
Stage #1: isopropyl 2-bromo-2‑methylpropanoate; 4-chloro-4'-hydroxybenzophenone With potassium carbonate at 145 - 155℃; for 4h; Inert atmosphere;
Stage #2: cholin hydroxide under 760.051 Torr;
68%
Stage #1: isopropyl 2-bromo-2‑methylpropanoate; 4-chloro-4'-hydroxybenzophenone With potassium carbonate at 145 - 155℃; for 3 - 6h;
Stage #2: cholin hydroxide In propan-1-ol; water for 3h; Product distribution / selectivity; Heating / reflux;
67.5%
fenofibric acid
42017-89-0

fenofibric acid

cholin hydroxide
123-41-1

cholin hydroxide

choline fenofibrate
856676-23-8

choline fenofibrate

Conditions
ConditionsYield
In methanol

856676-23-8Downstream Products

856676-23-8Relevant articles and documents

Phenoxy aromatic acid with cyclopropyl and pharmaceutically acceptable salt thereof as well as preparation method and application thereof

-

, (2021/07/17)

The invention provides phenoxy aromatic acid with cyclopropyl, a preparation method of the phenoxy aromatic acid, pharmaceutically acceptable salt of the phenoxy aromatic acid with cyclopropyl and a preparation method of the pharmaceutically acceptable salt, and further provides dosage forms of the phenoxy aromatic acid with cyclopropyl and the pharmaceutically acceptable salt of the phenoxy aromatic acid with cyclopropyl. The invention also discloses application of the compound in medicines for treating hyperlipidemia diseases. The compound provided by the invention has a relatively good blood fat reducing drug effect, so that the compound has a very good application prospect.

Interesting morphological behavior of organic salt choline fenofibrate: Effect of supersaturation and polymeric impurity

Bordawekar, Shailendra,Kuvadia, Zubin,Dandekar, Preshit,Mukherjee, Samrat,Doherty, Michael

, p. 3800 - 3812 (2014/08/18)

Crystal habit of drug molecules can have significant influence on the processing and performance of pharmaceutical products. During the development of Trilipix, a pharmaceutical product used for the treatment of mixed dyslipidemia, several crystal habits were observed for the active ingredient choline fenofibrate. The dissolution and performance of the drug product were not impacted by changes in crystal habit of the active ingredient due to high solubility of the drug. However, the formulation process was impacted by variations in crystal habit of the active ingredient, requiring robust control of the crystal habit. The crystal habit was greatly influenced by supersaturation during crystallization from a mixed solvent system comprising methanol and isopropanol. In addition to supersaturation, trace levels of a polymeric impurity in the starting material fenofibrate had a detrimental effect on the crystal habit. This article discusses the effects of these factors on the crystal habit of choline fenofibrate and the design of a crystallization process to deliver the target crystal habit, most suited to the formulation process. The article also provides preliminary mechanistic insights into the crystal habit of this organic salt using an extension of the spiral growth model for morphology prediction of organic molecular crystals. An attempt is made to explain the effect of supersaturation and impurity on the crystal habit of choline fenofibrate using the concepts of stability of surfaces, building units, periodic bond chain theory, and the spiral growth model.

AN IMPROVED PROCESS FOR THE PREPARATION OF CHOLINE SALT OF FENOFIBRIC ACID AND ITS NOVEL POLYMORPH

-

Page/Page column 7, (2010/08/09)

The present invention relates to an improved process for the preparation of choline salt of fenofibric acid corresponding to formula (I). The present invention also provides crystalline polymorphic form of choline salt of fenofibric acid corresponding to formula (I) designated as form A.

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