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ChemicalBook CAS DataBase List (2S,3R)-2-((S)-1-(3,5-bis(trifluoroMethyl)phenyl)ethoxy)-3-(4-fluorophenyl)Morpholine

(2S,3R)-2-((S)-1-(3,5-bis(trifluoroMethyl)phenyl)ethoxy)-3-(4-fluorophenyl)Morpholine synthesis

5synthesis methods
-

Yield:-

Reaction Conditions:

with hydrogen;5% palladium over charcoal in methanol at 30; for 3 h;

Steps:

24

EXAMPLE 24: PREPARATION OF THE COMPOUND OF FORMULA IIIa 16 g of the compound of Formula IVa obtained from Example 23 , 16 g of 5% palladium on carbon, and 160 ml of methanol were charged into a clean and dry hydrogenation vessel. Dry hydrogen gas of pressure 3.0 kg/cm2 was passed into the reaction suspension for a period of 3 hours at about 30 0C. After the EPO completion of the reaction, reaction suspension was filtered through celite and was washed with 80 ml of methanol. The resultant filtrate was distilled completely under vacuum to afford a crude syrup (Formula IIIa). 100 ml of acetonitrile was charged to the residue, left overnight and the separated solid was filtered to obtain 5 g of the title compound.Specific optical rotation: [α]D=0.00° ( C= 1% MeOH);Purity by RS HPLC: A8B7 at retention time (RT) 17.1 minutes: 87.39%, A7B8 at retention time (RT) 19.2 minutes: 8.23%.

References:

WO2007/44829,2007,A2 Location in patent:Page/Page column 43

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