Landiolol hydrochloride

Landiolol hydrochloride Basic information
Product Name:Landiolol hydrochloride
Synonyms:[(4S)-2,2-dimethyl-1,3-dioxolan-4-yl]methyl 3-[4-[(2S)-2-hydroxy-3-[2-(morpholine-4-carbonylamino)ethylamino]propoxy]phenyl]propanoate hydrochloride;Landiolol hydrochloride;Benzenepropanoic acid, 4-(2-hydroxy-3-((2-((4-morpholinylcarbonyl)amino)ethyl)amino)propoxy)-, (2,2-dimethyl-1,3-dioxolan-4-yl)methyl ester, (S-(R*,R*))-, hydrochloride;Ono 1101 hydrochloride;-2,2-Dimethyl-1,3-dioxolan-4-yl);-2-hydroxy-3-((2-(morpholine-4-carboxamido);methyl 3-(4-((S);propanoate hydrochloride
CAS:144481-98-1
MF:C25H40ClN3O8
MW:546.06
EINECS:1308068-626-2
Product Categories:APIs;API;144481-98-1
Mol File:144481-98-1.mol
Landiolol hydrochloride Structure
Landiolol hydrochloride Chemical Properties
Melting point 125.4°
storage temp. Refrigerator
solubility DMSO (Slightly), Ethanol (Slightly, Sonicated)
form Solid
color White to Off-White
Safety Information
RTECS DA8346700
HS Code 2934.99.4700
ToxicityLD50 in mice (mg/kg): 290 i.v. (Iguchi)
MSDS Information
Landiolol hydrochloride Usage And Synthesis
DescriptionLandiolol hydrochloride (14) was launched in Japan by Ono for the treatment of intraoperative tachyarrhythmia. It improves tachyarrhythmia by selectively blocking β1 receptors located mainly in the heart and by inhibiting the action of catecholamine.
UsesLandiolol is an ultra-short acting beta blocker that is used to treat patients with cardiac arrhythmias and is also used to treat tachycardia during anasthesia.
DefinitionChEBI: Landiolol hydrochloride is a member of morpholines.
SynthesisThe synthesis of landiolol appeared in an earlier patent in 1990. Esterification of 3- (4-hydroxyphenyl)propionic acid (141) with 2,2-dimethyl- 1,3-dioxolan-4-ylmethyl chloride (142) in DMSO gave desired ester 143 in 57% yield. Treatment of phenol 143 with bromo epoxide 144 in the present of K2CO3 afforded ether 145 in 76% yield. Epoxide 145 was then reacted with free amine 146 via a neucleophilic ring opening process to provide landiolol (14).

Synthesis_144481-98-1

Landiolol hydrochloride Preparation Products And Raw materials
Raw materialsLandiolol
Palonosetron Hydrochloride Levofloxacin HCL Capsule Ulipristal Acetate Cetirizine hydrochloride Urapidil hydrochloride Cefazedone sodium salt DRONEDARONE HYDROCHLORIDE 1-AdaMantanethylaMine Sildenafil citrate Tropisetron hydrochloride Landiolol

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