A kind of preparation method of landylol oxalate

A compound and weight technology, applied in the preparation of an important intermediate product of landiolol hydrochloride, the field of preparation technology of landiolol oxalate, can solve the problem of difficult to use pharmaceutical injection preparations, unfavorable industrialized production, low product yield, etc. problem, to avoid alcoholysis, low cost, simple operation effect
CN104003973BActive Publication Date: 2016-02-24ZEIN BIOTECHNOLOGY CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
ZEIN BIOTECHNOLOGY CO LTD
Publication Date
2016-02-24

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Abstract

The invention discloses a method for preparing landilol oxalate, the preparation method comprising: (2,2-dimethyl-1,3-dioxolan-4S-yl)methyl -3-[4-(2(S),3-epoxypropyl)phenyl]propionate (compound of formula II) and N-(2-aminoethyl)-4-morpholine carboxamide oxalate (Compound of formula III) as a raw material, undergoes a ring-opening reaction in a suitable solvent to obtain [(4S)-2,2-dimethyl-1,3-dioxolan-4-yl]methyl 3-[4 -[(2S)-2-Hydroxy-3-[2-(morpholine-4-carboxamido)ethylamino]propoxy]phenyl]propionate oxalate (compound of formula I). The synthesis process of the invention has the advantages of mild reaction conditions, simple operation, low cost, high product yield, good quality, etc., and is suitable for industrialized production.
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Description

technical field

[0001] The invention belongs to the technical field of medicinal chemistry, and relates to a preparation process of landisolol oxalate, which is an important intermediate product for preparing landisolol hydrochloride. Background technique

[0002] During surgery, various stimuli to the body due to endotracheal intubation, extubation, skin incision, and surgical operations cause sympathetic nerve excitement, release excess catecholamines, increase heart rate, and easily lead to tachycardia. out of order. Especially in patients with ischemic heart disease and high blood pressure, the load on the heart will be increased just because of the increase in the heart rate, thereby causing coronary ischemia. Therefore, anesthesia surgery, especially in patients with ischemic heart disease or hypertension, has great risks. According to literature reports, even in countries with advanced medical facilities and technologies such as Europe and the United States, the inc...

Claims

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