ChemicalBook CAS DataBase List Landiolol hydrochloride

Landiolol hydrochloride synthesis

6synthesis methods

Product Name:Landiolol hydrochloride
CAS Number:144481-98-1
Molecular formula:C25H40ClN3O8
Molecular Weight:546.06

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).

133242-30-5 Synthesis

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Yield:144481-98-1 95.9%

Reaction Conditions:

with hydrogenchloride in ethyl acetate at 5 - 10; for 2 h;

Steps:

1.6 Preparation of Lantilolol Hydrochloride

Add Lantilolol (10g, 19.62mmol) and 100mL of ethyl acetate to the reaction flask. The temperature of the ice-water bath is lowered below 5 ° C, and a temperature of 10-18 ° C is added dropwise to a 15-18% HCl-ethyl acetate solution 4.63g A large amount of solid was gradually precipitated, dripped, stirred below 10 ° C for 2h, filtered, washed with ethyl acetate, and dried under vacuum at 50 ° C to obtain 10.28 g of a white solid with a yield of 95.9% and an HPLC purity of 99.85%.

References:

CN110483470,2019,A Location in patent:Paragraph 0031; 0045-0047