Sarpogrelate hydrochloride synthesis
- Product Name:Sarpogrelate hydrochloride
- CAS Number:135159-51-2
- Molecular formula:C24H32ClNO6
- Molecular Weight:465.967
108-30-5
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![1-(Dimethylamino)-3-[2-[2-(3-methoxyphenyl)ethyl]phenoxy]-2-propanol hydrochloride](/CAS/GIF/135261-74-4.gif)
135261-74-4
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135159-51-2
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Yield:135159-51-2 95.4%
Reaction Conditions:
Stage #1: (±)-1-{2-[2-(3-methoxyphenyl)ethyl]-phenoxy}-3-(dimethylamino)-2-propanol hydrochloridewith sodium hydroxide in dichloromethane;water;
Stage #2: succinic acid anhydride in tetrahydrofuran at 35 - 40;
Stage #3: with hydrogenchloride in water; pH=3; for 1 h;
Steps:
3 Step 3: Preparation of Crude Sapogrylate Hydrochloride
Methylene chloride was added to the reactor, and 1-dimethylamino-3-(2-(2-(3-methoxyphenyl) ethyl)phenoxy)propan-2-ol hydrochloride prepared in step 2 was added. After adding an aqueous sodium hydroxide solution, the mixture was stirred and the layers were separated to remove the aqueous layer. Sodium sulfate was added to the organic layer, stirred for 30 minutes, filtered to remove moisture, and washed with methylene chloride. Then, it is filtered and concentrated under reduced pressure.Tetrahydrofuran and succinic anhydride were added to the reactor and stirred at 35 to 40°C. Confirm by TLC, and when the reaction is complete, it is concentrated under reduced pressure.Add ethyl acetate and isopropanol and cool. The pH was adjusted to 3.0±0.2 by adding hydrochloric acid, and stirred for about 1 hour.The resulting crystals were filtered and washed with ethyl acetate.Dry for about 7 hours or more in a dryer to obtain crude sapogrylate hydrochloride.
References:
KR2020/99018,2020,A Location in patent:Paragraph 0084; 0086-0090; 0158
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135963-42-7
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135159-51-2
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![2-[2-(3-Methoxyphenyl)ethyl]phenol](/CAS/GIF/167145-13-3.gif)
167145-13-3
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135159-51-2
245 suppliers
$37.00/5mg