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CasNo: 518048-02-7
MF: C24H25FN4O5
Appearance: off-white solid
InChI:InChI=1/C24H25FN4O5/c1-24(2,28-23(33)34-14-16-7-5-4-6-8-16)22-27-18(19(30)21(32)29(22)3)20(31)26-13-15-9-11-17(25)12-10-15/h4-12,30H,13-14H2,1-3H3,(H,26,31)(H,28,33)
The present work describes a two-step pr...
Raltegravir sodium synthesis was achieve...
The invention discloses a novel and sele...
Multiple sources of anticipated degradat...
2-(1-benzyloxycarbonylamino-1-methyl-ethyl)-5-hydroxy-1-methyl-6-oxo-1,6-dihydro-pyrimidine-4-carboxylic acid methyl ester
para-fluorobenzylamine
{1-[4-(4-fluoro-benzylcarbamoyl)-5-hydroxy-1-methyl-6-oxo-1,6-dihydro-pyrimidin-2-yl]-1-methyl-ethyl}carbamic acid benzyl ester
Conditions | Yield |
---|---|
In
ethanol;
at 4 - 72 ℃;
for 4h;
|
90% |
2-(1-benzyloxycarbonylamino-1-methyl-ethyl)-5-hydroxy-1-methyl-6-oxo-1,6-dihydro-pyrimidine-4-carboxylic acid methyl ester; para-fluorobenzylamine;
In
ethanol;
at 4 - 72 ℃;
for 5h;
In
ethanol; water;
at 60 ℃;
|
90% |
In
ethanol;
at 4 - 72 ℃;
for 4h;
|
90% |
In
ethanol;
at 4 - 72 ℃;
for 4h;
|
90% |
In
ethanol;
at 4 - 72 ℃;
for 4.75h;
|
90% |
In
ethanol;
at 0 - 72 ℃;
for 4.25h;
Large scale reaction;
|
90% |
In
methanol;
at 60 - 65 ℃;
|
|
2-(1-benzyloxycarbonylamino-1-methyl-ethyl)-5-hydroxy-1-methyl-6-oxo-1,6-dihydro-pyrimidine-4-carboxylic acid methyl ester; para-fluorobenzylamine;
In
ethanol;
for 3h;
Reflux;
With
acetic acid;
In
ethanol; water;
|
13.2 g |
{1-[4-(4-fluoro-benzylcarbamoyl)-5,6-dihydroxy-pyrimidin-2-yl]-1-methyl-ethyl}-carbamic acid benzyl ester
trimethylsulfoxonium iodide
{1-[4-(4-fluoro-benzylcarbamoyl)-5-hydroxy-1-methyl-6-oxo-1,6-dihydro-pyrimidin-2-yl]-1-methyl-ethyl}carbamic acid benzyl ester
Conditions | Yield |
---|---|
With
magnesium hydroxide;
In
1-methyl-pyrrolidin-2-one; water;
at 97 - 109 ℃;
for 6.5h;
|
89% |
With
magnesium hydroxide;
In
water;
at 100 ℃;
|
89% |
2-(1-benzyloxycarbonylamino-1-methyl-ethyl)-5-hydroxy-1-methyl-6-oxo-1,6-dihydro-pyrimidine-4-carboxylic acid methyl ester
para-fluorobenzylamine
{1-[4-(4-fluoro-benzylcarbamoyl)-5,6-dihydroxy-pyrimidin-2-yl]-1-methyl-ethyl}-carbamic acid benzyl ester
trimethylsulfoxonium iodide
ethyl (2-(4-(4-fluorobenzylcarbamoyl)-1,6-dihydro-5-hydroxy-1-methyl-6-oxopyrimidin-2-yl)propan-2-ylcarbamoyl)formate