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A kind of preparation method of mosapride intermediate

A technology for intermediates and compounds, applied in the field of preparation of mosapride intermediates, can solve the problems of prolonging the process route, increasing the time of mosapride citrate, capital consumption, high price and the like

Active Publication Date: 2021-04-09
SHANGHAI HANSOH BIOMEDICAL +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0012] It can be seen that the intermediate 2-(4-fluorobenzylamino)ethanol is required to be used in the synthetic route of the intermediate I disclosed in the prior art. The extension of the process route increases the time and capital consumption of preparing mosapride citrate

Method used

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  • A kind of preparation method of mosapride intermediate
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  • A kind of preparation method of mosapride intermediate

Examples

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Comparison scheme
Effect test

Embodiment 1

[0061] Example 1 Preparation of 2-(2-hydroxyl-3-((2-hydroxyethyl)amino)propyl)isoindoline-1,3-dione

[0062]

[0063] Add phthalimide potassium salt (370.0g, 2mol) and 2L of absolute ethanol into the reaction flask, heat to 65°C and stir to dissolve. After the material is dissolved, add dichloroisopropanol (0.229L, 2.4mol), Triethylamine (0.557L, 4mol), reflux reaction for 6 hours to generate intermediate N-(2-hydroxyl-3-chloropropyl)phthalimide, lowered to room temperature, added 2-aminoethanol ( 0.241L, 4mol), heated up to 50°C and reacted for 6 hours, evaporated the ethanol to dryness under reduced pressure, added 10L each of ethyl acetate and water, separated the liquid, washed the water phase twice with ethyl acetate, washed the organic phase twice with water, and combined The organic phase was dried over anhydrous magnesium sulfate, filtered with suction, and evaporated to dryness under reduced pressure to obtain 472 g of a white solid, namely 2-(2-hydroxyl-3-((2-hydr...

Embodiment 2

[0064] Example 2 Preparation of 2-(2-hydroxyl-3-((2-hydroxyethyl)amino)propyl)isoindoline-1,3-dione

[0065]

[0066] Add phthalimide potassium salt (370.0g, 2mol) and 2L of absolute ethanol into the reaction flask, heat to 65°C and stir to dissolve. After the material is dissolved, add dichloroisopropanol (0.229L, 2.4mol), DMAP (0.539L, 4mol), reflux reaction 6 hours generates intermediate N-(2-hydroxyl-3-chloropropyl) phthalimide, is down to room temperature, adds 2-aminoethanol (0.241L , 4mol), heated up to 50°C and reacted for 6 hours, evaporated the ethanol to dryness under reduced pressure, added 10L each of ethyl acetate and water, separated the layers, washed the aqueous phase twice with ethyl acetate, washed the organic phase twice with water, and combined the organic phases , dried over anhydrous magnesium sulfate, suction filtered, and evaporated to dryness under reduced pressure to obtain a white solid that is 2-(2-hydroxyl-3-((2-hydroxyethyl)amino)propyl)isoind...

Embodiment 3

[0067] Example 3 Preparation of 2-(2-hydroxyl-3-((2-hydroxyethyl)amino)propyl)isoindoline-1,3-dione

[0068]

[0069] Add phthalimide potassium salt (370.0g, 2mol) and DMSO 2L into the reaction flask, heat to 65°C and stir to dissolve, add dichloroisopropanol (0.229L, 2.4mol), triethyl Amine (0.557L, 4mol), reflux reaction for 6 hours to generate intermediate N-(2-hydroxy-3-chloropropyl)phthalimide, lowered to room temperature, added 2-aminoethanol (0.241L , 4mol), heated up to 50°C and reacted for 6 hours, evaporated the ethanol to dryness under reduced pressure, added 10L each of ethyl acetate and water, separated the layers, washed the aqueous phase twice with ethyl acetate, washed the organic phase twice with water, and combined the organic phases , after drying over anhydrous magnesium sulfate, suction filtration, and evaporated to dryness under reduced pressure to obtain a white solid, namely 2-(2-hydroxyl-3-((2-hydroxyethyl)amino)propyl)isoindoline-1 , 3-diketone 46...

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Abstract

The invention discloses a preparation method of mosapride intermediate I. It comprises the following steps: phthalimide potassium salt reacts with dichloroisopropanol to generate N-(2-hydroxy-3-chloropropyl) phthalimide, and then condenses with 2-aminoethanol After cyclization, the intermediate 2-aminomethylmorpholine is obtained, and further reacted with 4-fluorobenzyl chloride under alkali conditions to obtain the mosapride intermediate I. This method has low cost and high reaction purity, and is suitable for industrial operation; .

Description

technical field [0001] The invention relates to the field of medicine and chemical industry, in particular to a preparation method of a mosapride intermediate. Background technique [0002] Mosapride Citrate is a selective serotonin 4 (5-HT4) receptor agonist, which can promote the release of acetylcholine, stimulate the gastrointestinal tract and exert a prokinetic effect, thereby improving function Gastrointestinal symptoms in patients with sexual dyspepsia, but does not affect the secretion of gastric acid. The chemical name is 4-amino-5-chloro-2-ethoxy-N-[[4-(4-fluorobenzyl)-2-morpholinyl]methyl]benzamide citrate dihydrate , CAS number: 156925-25-6, has the following structure: [0003] [0004] The production preparation technology of existing mosapride citrate is more complicated, and each step intermediate affects the quality of final product, especially intermediate I 4-(4-fluorobenzyl)-2-aminomethylmorpholine, intermediate The purity of intermediate I is low, ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D265/30
CPCC07D265/30
Inventor 张春林钟春华孙晶晶宗书敏
Owner SHANGHAI HANSOH BIOMEDICAL
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