Risperidone synthesis
- Product Name:Risperidone
- CAS Number:106266-06-2
- Molecular formula:C23H27FN4O2
- Molecular Weight:410.48
63234-80-0
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84163-13-3
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106266-06-2
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Yield:106266-06-2 93.2%
Reaction Conditions:
with sodium carbonate in water at 110 - 120; for 0.666667 h;Product distribution / selectivity;
Steps:
9
Example 9; Preparation of 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)piperidin-1-yl]ethyl]-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidin-4-one (risperidone)In a 50-ml reaction flask, 2.56 g of 6-fluoro-3-(4-piperidinyl)-1,2-benzisoxazole hydrochloride and 2.95 g of 3-(2-chloroethyl)-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidin-4-one are placed, then a sodium carbonate solution or suspension (dissolved or suspended 8.5 g of sodium carbonate in 25 ml water) is added. The mixture is put into heating bath at 110-120° C. with stirring for 40 min, then cooled with continuous stirring to the room temperature and the precipitate solid is filtered, washed with pure water, and dried to give 3.82 g of the product in 93.2% yield. The product is purified to obtain a purity of 99.5% (determined by HPLC) with DMF and isopropanol.
References:
Zhang, Guiling;Zhu, Yidong;Fan, Chuanwen;Zhang, Minghui;Wang, Jingyi US2010/130740, 2010, A1 Location in patent:Page/Page column 4
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106266-06-2
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158697-66-6
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84163-13-3
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106266-06-2
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106266-06-2
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