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Purity:99%
The invention relates to a preparation m...
The invention provides a synthesis metho...
A NK 1 antagonist having the formula (I...
This application discloses a novel proce...
C42H44F6N2O5
Rolapitant
| Conditions | Yield |
|---|---|
|
With
palladium 10% on activated carbon; hydrogen;
In
methanol;
at 20 ℃;
under 3800.26 Torr;
Autoclave;
Large scale;
|
92.9% |
(S)-1-bromo-1-[3,5-bis(trifluoromethyl)phenyl]ethane
(5S,8S)-8-hydroxymethyl-8-phenyl-7-trifluoroacetyl-1,7-diazaspiro[4.5]nonan-2-one
Rolapitant
| Conditions | Yield |
|---|---|
|
(5S,8S)-8-hydroxymethyl-8-phenyl-7-trifluoroacetyl-1,7-diazaspiro[4.5]nonan-2-one;
With
sodium hydride;
In
N,N-dimethyl acetamide;
at 0 - 5 ℃;
for 0.5h;
(S)-1-bromo-1-[3,5-bis(trifluoromethyl)phenyl]ethane;
In
N,N-dimethyl acetamide;
|
90% |
methyl 3-[(3S,6S)-6-({(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy}methyl)-3-nitro-6-phenylpiperidin-3-yl]propanoate methylsulfonate
C36H40F6N2O6
C30H27F6NO4
(5S,8S)-8-[{(1R)-1-(3,5-bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one maleate
(5S,8S)-8-[{(1R)-1-(3,5-bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one mesylate
(5S,8S)-8-[{(1R)-1-(3,5-bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one oxalate
(5S,8S)-8-[{(1R)-1-(3,5-bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one esylate
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