183814-30-4

Usage

Uses

Used in Pharmaceutical Industry:
Formoterol Fumarate Dihydrate is used as a selective β2-adrenergic receptor agonist for the treatment of asthma and chronic obstructive pulmonary disease (COPD). It helps to relax the muscles in the airways and increase air flow to the lungs, providing relief from shortness of breath and other respiratory symptoms.
Used in Respiratory Applications:
Formoterol Fumarate Dihydrate is used as an antiasthmatic agent to manage and prevent asthma attacks. Its selective action on β2-adrenergic receptors helps to reduce inflammation and constriction in the airways, improving lung function and overall respiratory health.

Biological Activity

Potent, selective and long-acting β 2 -adrenoceptor agonist. Displays 330-fold selectivity for β 2 over β 1 receptors (pK d values are 8.12 and 5.58 respectively). Potently relaxes guinea pig trachea (pD 2 = 9.29), and is longer-acting and 100-fold more potent than salbutamol.

Biochem/physiol Actions

β2-Adrenoreceptor agonist.

InChI:InChI=1/C19H24N2O4.C4H4O4.2H2O/c1-13(9-14-3-6-16(25-2)7-4-14)20-11-19(24)15-5-8-18(23)17(10-15)21-12-22;5-3(6)1-2-4(7)8;;/h3-8,10,12-13,19-20,23-24H,9,11H2,1-2H3,(H,21,22);1-2H,(H,5,6)(H,7,8);2*1H2/b;2-1+;;/t13-,19+;;;/m1.../s1

Upstream product

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Relevant academic research and scientific papers

Preparation method and application of formoterol and medicinal salt thereof

The invention provides a preparation method and application of formoterol and medicinal salt thereof, and relates to the technical field of chemical synthesis. The preparation method of formoterol comprises the following steps: reacting a compound shown as a formula I under the action of a palladium-containing catalyst, a hydrogen donor and an alkali reagent to obtain a compound shown as a formulaII, wherein the hydrogen donor is a combination of formic acid and ammonium formate. The compound shown in the formula I contains O-benzyl, N-benzyl, formyl and methoxyl at the same time, hydrogen can be slowly and continuously generated under the action of a palladium-containing catalyst by adopting the combination of a hydrogen donor and an alkali reagent, a method for directly introducing hydrogen in the conventional technology is replaced, benzyl of O-benzyl and N-benzyl on the compound shown in the formula I can be removed, formyl and methoxyl are not affected, the yield and purity of the product are guaranteed, reaction conditions are mild, technological operation is safe and easy to control, and the method is simple, convenient and easy to implement and suitable for large-scale production.

AN IMPROVED PROCESS FOR THE PREPARATION OF HIGH PURITY FORMOTEROL AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS

The present invention relates to an improved process for the preparation of high purity formoterol and its pharmaceutically acceptable salts of Formula-I(C).

Novel aerosol formulation containing a polar fluorinated molecule

The present invention relates to a stable pharmaceutical aerosol formulation intended for inhalation. The formulation contains an active substance, an aerosol propellant, a polar flurorinated molecule and an excipient. The preferred propellant is HFA 134a or HFA 227 or a mixture thereof.