Landiolol hydrochloride

CAS No.：144481-98-1

Important Notice

This product is a chemical product/pharmaceutical intermediate. It is not a drug, an active pharmaceutical ingredient (API), or a pharmaceutical-grade material. It has not been granted a drug approval number or a Chemical Drug Substance Approval Notice, has not passed drug-related review and approval, and is not manufactured, tested, or released in accordance with pharmaceutical GMP.
This product is intended solely for non-clinical research, process development, quality studies, further chemical processing, or chemical synthesis. It must not be used in drug-product manufacturing, clinical trials, clinical diagnosis, or administration to humans or animals, or be sold, used as an input, submitted for regulatory filing, or released as an API or pharmaceutical material.
The purchaser must not use this product, or supply it to another party, for personal consumption, sports or fitness, weight loss, health supplements, food, or animal feed.

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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
Mol File:	144481-98-1.mol

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
Toxicity	LD50 in mice (mg/kg): 290 i.v. (Iguchi)

MSDS Information

Landiolol hydrochloride Usage And Synthesis

Description	Landiolol 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.
Uses	Landiolol 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.
Synthesis	The 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).

Landiolol hydrochloride Preparation Products And Raw materials

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