ChemicalBook CAS DataBase List Mosapride citrate

Mosapride citrate synthesis

11synthesis methods

Product Name:Mosapride citrate
CAS Number:112885-42-4
Molecular formula:C27H33ClFN3O10
Molecular Weight:614.02

112885-41-3

112885-42-4

GENERAL STEPS: To a suspension of 1.3 g (2.5 mmol) of 4-amino-5-chloro-2-ethoxy-N-((4-(4-fluorobenzyl)morpholin-2-yl)methyl)benzamide (Compound VIII) and 3 mL of water was added 12 mL of 117% aqueous hydrochloric acid. The resulting solution was stirred at 40°C for 3 hours, cooled to 10°C and 38 mL of 4M aqueous sodium hydroxide solution was added dropwise. The precipitated mosapride base (Compound IX) was filtered and washed twice with water to give 1.05 g (100%) of Compound IX.1.01 g of the above obtained Compound IX was warmed to boiling with 25 mL of 10% aqueous citric acid solution with stirring, cooled to 0°C, the precipitated product was filtered, and washed twice with water to give 1.34 g (86%) of 4-amino-5-chloro-2-ethanol oxy-N-((4-(4-fluorobenzyl)morpholin-2-yl)methyl)benzamide 2-hydroxypropane-1,2,3-tricarboxylate. Melting point: 110-113°C.

112885-41-3
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77-92-9 Synthesis

77-92-9
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112885-42-4
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Yield:112885-42-4 97.2%

Reaction Conditions:

in ethanol;water at 70 - 75; for 0.5 h;Temperature;

Steps:

1-2 Example 2

68.8 g of Mosapride Base was added to 205 mL of ethanol and dissolved under reflux for 30 minutes. 34.4 g of anhydrous citric acid was dissolved in 410 mL of purified water, added dropwise, and 10 mg of Mosapride citric acid dihydrate seed was added while maintaining the temperature at 70 to 75°C, followed by stirring for 30 minutes to prepare a reaction product. The reaction was first cooled to 50° C. and stirred for 2 hours. Then, the reaction was cooled again to 35° C. and stirred for 1 hour. Finally, the reaction was cooled for 3 times to 5° C. and stirred for 2 hours. The precipitated crystals were filtered and washed with a mixture of 20 mL of ethanol and 40 mL of purified water to obtain 103.1 g of Mosapride citrate dihydrate (MSP-CRY-02) crystals of uniform particle size and high purity (99.9%) (yield: 97.2%) )

References:

KR2020/99016,2020,A Location in patent:Paragraph 0121-0145

112885-41-3
187 suppliers
$5.00/10mg

112885-42-4
265 suppliers
$10.00/10mg

References