- Umeclidinium Bromide
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- $0.00 / 1Kg/Bag
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2024-04-22
- CAS:869113-09-7
- Min. Order: 1Kg/Bag
- Purity: 0.99
- Supply Ability: 20 tons
- Umeclidinium bromide
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- $5.00 / 1KG
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2024-04-16
- CAS:869113-09-7
- Min. Order: 1KG
- Purity: 99%
- Supply Ability: g-kg-tons, free sample is available
- Umeclidinium bromide
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- $10.00 / 1kg
-
2024-04-02
- CAS:869113-09-7
- Min. Order: 1kg
- Purity: 99%
- Supply Ability: 100 tons
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| | Umeclidinium bromide Basic information |
| Product Name: | Umeclidinium bromide | | Synonyms: | 1-(2-(benzyloxy)ethyl)-4-(hydroxydiphenylmethyl)quinuclidin-1-ium bromide;GSK573719A;UMeclidiniuM broMide;UMeclidiuM;UMeclidiniuM BroMide (API);4-[Hydroxy(diphenyl)methyl]-1-[2-[(phenylmethyl)oxy]ethyl]-1-azoniabicyclo[2.2.2]octane bromide;1-Azoniabicyclo[2.2.2]octane, 4-(hydroxydiphenylMethyl)-1-[2-(phenylMethoxy)ethyl]-, broMide (1:1);umeclidinium | | CAS: | 869113-09-7 | | MF: | C29H34BrNO2 | | MW: | 508.48976 | | EINECS: | 638-761-1 | | Product Categories: | API;869113-09-7 | | Mol File: | 869113-09-7.mol |  |
| | Umeclidinium bromide Chemical Properties |
| Melting point | >231°C (dec.) | | storage temp. | under inert gas (nitrogen or Argon) at 2-8°C | | solubility | DMSO (Slightly), Methanol (Slightly), Water (Slightly) | | form | Solid | | color | White to Off-White | | Stability: | Hygroscopic |
| | Umeclidinium bromide Usage And Synthesis |
| Description | Umeclidinium bromide is a long-acting muscarinic acetylcholine
antagonist developed by GlaxoSmithKline and approved
by the US FDA at the end of 2013 for use in combination with
vilanterol, a b2 agonist, for the treatment of chronic obstructive
pulmonary disease. Due to umeclidinium’s poor oral bioavailability,
the drug is administrated by inhalation as dry powder. | | Uses | Umeclidinium Bromide is considered as a potentially long-acting antimuscarinic agent. | | Definition | ChEBI: A quaternary ammonium salt that is the bromide salt of umeclidinium. Used in combination with vilanterol for long-term maintenance treatment of airflow obstruction in patients with chronic obstructive pulmonary disease. | | Synthesis | Commercially available ethyl isonipecotate (278) was alkylated
with 1-bromo-2-chloroethane in the presence of K2CO3 in acetone
to give ethyl 1-(2-chloroethyl)piperidine-4-carboxylate (279). This
material was then treated with lithium diisopropylamine (LDA) in
THF to affect a transannular substitution reaction resulting in the
cyclized quinuclidine 280 in 96% yield. Excess of phenyllithium
was added to ester 280 in THF starting at low temperature then
gradually warming to room temperature to give tertiary alcohol 281 in 61% yield. Amine 281 was finally alkylated with benzyl 2-
bromoethyl ether (282) in MeCN/CHCl3 at elevated temperatures
to afford umeclidinium bromide (XXXV) in 69% yield. 
| | references | [1] salmon m, luttmann m a, foley j j, et al. pharmacological characterization of gsk573719 (umeclidinium): a novel, long-acting, inhaled antagonist of the muscarinic cholinergic receptors for treatment of pulmonary diseases. journal of pharmacology and experimental therapeutics, 2013, 345(2): 260-270. |
| | Umeclidinium bromide Preparation Products And Raw materials |
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