- 287930-73-8
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- $100.00 / 100kg
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2025-09-17
- CAS:287930-73-8
- Min. Order: 100kg
- Purity: 99.99%
- Supply Ability: 100Tons
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| | 4-BENZYL-2-HYDROXY-MORPHOLIN-3-ONE Basic information |
| Product Name: | 4-BENZYL-2-HYDROXY-MORPHOLIN-3-ONE | | Synonyms: | Aprepitant Impurity 48;Fosaprepitant Impurity 23;4-BENZYL-2-HYDROXY-MORPHOLIN-3-ONE;3-Morpholinone,2-hydroxy-4-(phenylMethyl)-;2-Hydroxy-4-(phenylMethyl)-3-Morpholinone;Fosaprepitant Impurity B;-2-hydroxymorphoL;Aprepitant intermediates，4-Benzyl-2-hydroxy-morpholin-3-one | | CAS: | 287930-73-8 | | MF: | C11H13NO3 | | MW: | 207.23 | | EINECS: | 811-794-0 | | Product Categories: | pharmacetical | | Mol File: | 287930-73-8.mol |  |
| | 4-BENZYL-2-HYDROXY-MORPHOLIN-3-ONE Chemical Properties |
| Melting point | 134.0 to 138.0 °C | | Boiling point | 441.7±45.0 °C(Predicted) | | density | 1.292±0.06 g/cm3(Predicted) | | storage temp. | Sealed in dry,Room Temperature | | solubility | DMSO (Slightly), Methanol (Slightly, Heated) | | form | Solid | | pka | 11.00±0.20(Predicted) | | color | White to Off-White | | Optical Rotation | 0.30°(C=0.01g/ml CHCL3) |
| | 4-BENZYL-2-HYDROXY-MORPHOLIN-3-ONE Usage And Synthesis |
| Uses | 2-Hydroxy-4-(phenylmethyl)-3-morpholinone, is an intermediate used for the synthesis of NK1 Receptor Antagonist Aprepitant (A729800), used as as antiemetic drugs. | | Synthesis | A 50% aqueous solution of glyoxalate (67 mL, 0.61 mol) and tetrahydrofuran (130 mL) were added to a 250 mL round bottom flask and heated to reflux. A solution of N-benzylethanolamine (41.5 g, 0.27 mol) in tetrahydrofuran (20 mL) was slowly added dropwise under reflux conditions. After completion of the reaction, the tetrahydrofuran solvent was removed by rotary evaporator. Water (170 mL) was added to the residue, stirred and cooled to room temperature, followed by continued stirring in an ice water bath for 30 min to promote crystallization. The precipitated solid was collected by filtration and washed with ice water. The resulting pale yellow solid was dried to afford the target product 4-benzyl-2-hydroxy-morpholin-3-one (compound of formula VII, 51.8 g, 91% yield) with a melting point of 132-136 °C. | | References | [1] Patent: CN103030668, 2016, B. Location in patent: Paragraph 0031-0033
[2] Journal of the American Chemical Society, 2003, vol. 125, # 8, p. 2129 - 2135 |
| | 4-BENZYL-2-HYDROXY-MORPHOLIN-3-ONE Preparation Products And Raw materials |
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