Indacaterol

Indacaterol
Indacaterol
Indacaterol

Indacaterol

Min.Order / FOB Price:Get Latest Price

1 Kilogram

Negotiable

  • Min.Order :1 Kilogram
  • Purity: 99（%）
  • Payment Terms : L/C,D/A,D/P,T/T,Other

Keywords

Indacaterol 312753-06-3 C24H28N2O3

Quick Details

  • Appearance:white solid
  • Application:medical intermediate
  • PackAge:As required
  • ProductionCapacity:5|Metric Ton|Month
  • Storage:Kept in a well-closed, light-resistant,dry and cool place
  • Transportation:by sea or by air

Superiority:

Changzhou Xuanming Chemical Co., Ltd. is dedicated to the technology development, manufacturing, import and export chemicals, which are specialized in pharmaceutical intermediates, pesticide intermediate, industry of fine chemicals and custom synthesis. Now, we enjoy good reputation among customers and take favorable market share in domestic and at abroad.

Changzhou Xuanming Chemical CO., LTD is located in Northern Jiangshu Industry Park, we have modern manufacture bases and some laboratories, which can supply the key intermediate for your projects, and short your synthesis scheme and supply you a reference compound for bioassay or a high purity analytical standard. We have been abided by “treat technology as first, quality as basis, customers as God, and be honest and sincere”. It is our final aim to provide environmental and high technological products and meet customers’ requirements according to keep effors on developing new chemical fields.

Changzhou Xuanming Chemical CO., LTD promises to help you with heart and soul.

Details:

Indacaterol Basic information
Description Indication Mechanism of Action Toxicity
Product Name: Indacaterol
Synonyms: Indacaterol;5-[(1R)-2-[(5,6-Diethyl-2,3-dihydro-1H-inden-2-yl)amino]-1-hydroxyethyl]-8-hydroxyquinolin-2(1H)-one;Indacaterol-d3;(R)-5-(2-(5,6-diethyl-2,3-dihydro-1H-inden-2-ylaMino)-1-hydroxyethyl)-8-hydroxyquinolin-2(1H)-one, Maleate salt;Arcapta;5-[2-(5,6-Diethyl-2,3-dihydro-1H-inden-2-ylaMino)-(1R)-hydroxyethyl]-8-hydroxyquinolin-2(1H)-one;2(1H)-Quinolinone,5-[(1R)-2-[(5,6-diethyl-2,3-dihydro-1H-inden-2-yl)amino]-1-hydroxyethyl]-8-hydroxy-;(R)-5-(2-(5,6-Diethyl-2,3-dihydro-1H-inden-2-ylamino)-1-hydroxyethyl)-8-hydroxyquinolin-2(1H)-
CAS: 312753-06-3
MF: C24H28N2O3
MW: 392.5
EINECS: 691-091-1
Product Categories: Agonist;Amines;Aromatics;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;Inhibitors
Mol File: 312753-06-3.mol
Indacaterol Structure
 
Indacaterol Chemical Properties
density  1.27
 
Safety Information
MSDS Information
 
 
Indacaterol Usage And Synthesis
Description Indacaterol is a new, ultra-long-acting, rapid onset β(2)-adrenoceptor agonist that was developed by Novartis. The drug is used in managing and controlling chronic obstructive pulmonary disease (COPD) and asthma. The European Medicines Agency (EMA) approved indacaterol as a drug in 2009 under the Onbrez trade name while in the United States the Food and Drug Administration approved it under the trade name Arcapta in 2011. The drug is manufactured as its maleate salt form. Also, indacaterol is a chiral molecule; however, only the pure R-enantiomer is distributed.
Indication Indacaterol is used in the maintenance of airflow obstruction in individuals with COPD for the long term, including emphysema and chronic bronchitis.
Mechanism of Action By stimulating the adrenergic beta-2-receptors in the airways’ smooth muscles, indacaterol is able to cause relaxation, thus augmenting the diameter of the airways that are normally constricted in COPD and asthma. Because of its high affinity to the lipid draft domains in the membrane of the airways, it is long acting, therefore it slowly detaches from the receptors. It is rapid acting due to its high intrinsic characteristic.
Toxicity In case of an overdose of indacaterol, the expected signs and symptoms include excessive beta-adrenergic stimulation, hypotension, hypertension, nervousness, fatigue, hyperglycaemia, insomnia, and metabolic acidosis.
Description Inhaled β2 adrenoceptor agonists are effective in the management of asthma and COPD, primarily through their bronchodilating properties. These drugs induce bronchodilation by causing direct relaxation of airway smooth muscle through activation of adenylate cyclase, which in turn increases intracellular cAMP levels. Indacaterol is the newest β2 agonist to reach the market. It is an ultra-long-acting agent with a duration of action suitable for once-a-day dosing. Indacaterol is supplied as an aerosol formulation of its maleate salt and is administered via a dry powder inhaler device. It is specifically approved for once-daily maintenance treatment of airflow obstruction in adult patients with COPD. In preclinical models, indacaterol is close to a full agonist at the human b2 adrenoceptor (Emax = 73 ± 1% of isoprenaline′s maximal effect, pEC50 = 8.06 ±0.02) while salmeterol displays only partial efficacy (38 ±1%). The functional selectivity profile of indacaterol over β1 human adrenoceptors is similar to that of formoterol, whereas its β3 adrenoceptor selectivity profile is similar to that of formoterol and salbutamol.
Originator Novartis (United Kingdom)
Definition ChEBI: A monohydroxyquinoline that consists of 5-[(1R)-2-amino-1-hydroxyethyl]-8-hydroxyquinolin-2-one having a 5,6-diethylindan-2-yl group attached to the amino function. Used as the maleate salt for treatment of chronic obstructive pulmonary di ease.
Brand name Onbrez Breezhaler
Side effects The most commonly reported adverse events associated with indacaterol treatment were nasopharyngitis, upper respiratory tract infection, and headache and cough following inhalation. Adverse events were mild or moderate in most cases, and became less frequent with continued treatment.
Chemical Synthesis The chemical synthesis of indacaterol begins with a-chlorination of 5-acetyl-8-benzyloxy-2-quinolone with benzyltrimethylammonium dichloro-iodate. The resultant chloroketone is reduced with borane in tetrahydrofuran in the presence of the chiral boron catalyst R-tetrahydro-1-methyl-3,3-diphenyl-1H,3H-pyrrolo[1,2c][ 1,3,2]oxazaborole to produce the corresponding chlorohydrin intermediate in high enantiomeric excess. The chlorohydrin intermediate is cyclized to the corresponding epoxide by treatment with potassium carbonate, the epoxide is condensed with 5,6-diethylindan-2-amine, and the benzyl protecting group is removed by hydrogenolysis to produce indacaterol. The 5,6-diethylindan-2-amine intermediate is derived from 1,2-diethylbenzene via Friedel-Crafts acylation with 3-chloropropionyl chloride, cyclization of the resultant 3-chloro- 1-(3,4-diethylphenyl)-1-propanone by means of concentrated sulfuric acid to 5,6-diethylindan-1-one, oximation with butyl nitrite, and reduction of the oxime to an amine via treatment with hydrogen over palladium- carbon.
 
Indacaterol Preparation Products And Raw materials

 

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