4-Benzyl-2-hydroxy-morpholin-3-one

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4-Benzyl-2-hydroxy-morpholin-3-one manufacturers

  • 287930-73-8
  • 287930-73-8 pictures
  • $100.00
  • 2026-08-21
  • CAS:287930-73-8
  • Min. Order: 100kg
  • Purity: 99.99%
  • Supply Ability: 100Tons
4-Benzyl-2-hydroxy-morpholin-3-one Basic information
Product Name:4-Benzyl-2-hydroxy-morpholin-3-one
Synonyms:Fosaprepitant Impurity 23;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;TIANFUCHEM--287930-73-8--High purity 4-BENZYL-2-HYDROXY-MORPHOLIN-3-ONE factory price;4- benzyl -2- hydroxymorpholine -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 Structure
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
pka11.00±0.20(Predicted)
color White to Off-White
Optical Rotation0.30°(C=0.01g/ml CHCL3)
Safety Information
HS Code 2934.99.4400
MSDS Information
4-Benzyl-2-hydroxy-morpholin-3-one Usage And Synthesis
Uses2-Hydroxy-4-(phenylmethyl)-3-morpholinone, is an intermediate used for the synthesis of NK1 Receptor Antagonist Aprepitant (A729800), used as as antiemetic drugs.
Synthesis
Glyoxylic acid

298-12-4

N-Benzylethanolamine

104-63-2

4-BENZYL-2-HYDROXY-MORPHOLIN-3-ONE

287930-73-8

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
Raw materialsGlyoxylic acid-->N-Benzylethanolamine
Preparation ProductsAprepitant
Tag:4-Benzyl-2-hydroxy-morpholin-3-one(287930-73-8) Related Product Information
Fosaprepitant Benzyl Ester Aprepitant Aprepitant Fosaprepitant Impurity 6 (2R,3S)-2-[(1S)-1-[3,5-Bis(trifluoroMethyl)phenyl]ethoxy]-3-(4-fluorophenyl)Morpholine hydrochloride [2R-[2aR*),3a]-2-[1-[3,5-Bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholine (R)-1-[3,5-Bis(trifluoromethyl)phenyl]ethanol Aprepitant Fosaprepitant Impurity 5 5-(hydroxymethyl)-1,2-dihydro-1,2,4-triazol-3-one (S)-2-((R)-1-(3,5-bis(trifluoroMethyl)phenyl)ethoxy)-4-benzylMorpholin-3-one 1,1,1-Trimethoxy-2-chloroethane Aprepitant (2S,3R)-2-((S)-1-(3,5-bis(trifluoroMethyl)phenyl)ethoxy)-3-(4-fluorophenyl)Morpholine Benzyl dihydrogen phosphate (2R,3R)-2-[(1R)-1-[3,5-Bis(trifluoroMethyl)phenyl]ethoxy]-3-(4-fluorophenyl)Morpholine 4-Benzyl-2-hydroxy-morpholin-3-one 4-Benzyl-morpholin-3-one