The present invention belongs to the pha...
The invention relates to a pyridone-cont...
The invention relates to a preparation m...
The invention relates to a dibenzo seven...
7,8-difluoro-6,11-dihydrodibenzo[b,e]thiazepin-11-one
7,8-difluoro-6,11-dihydrodibenzo[b,e]thiazepine-11-ol
Conditions | Yield |
---|---|
With
sodium tetrahydroborate;
In
ethanol;
at 20 - 50 ℃;
for 5h;
Solvent;
Large scale;
|
98% |
With
sodium tetrahydroborate; sodium hydroxide;
In
water; isopropyl alcohol;
at 40 ℃;
for 1.5h;
|
97% |
With
sodium tetrahydroborate;
In
ethanol; water;
Cooling with ice;
|
97% |
With
sodium tetrahydroborate; sodium hydroxide;
In
isopropyl alcohol;
at 40 ℃;
for 2h;
|
97% |
With
sodium tetrahydroborate; water; sodium hydroxide;
In
isopropyl alcohol;
at 0 - 40 ℃;
|
97% |
With
methanol; sodium tetrahydroborate;
at 0 - 20 ℃;
for 0.333333h;
|
97.7% |
With
sodium tetrahydroborate; sodium hydroxide;
In
water; isopropyl alcohol;
at 40 ℃;
for 1.5h;
|
97% |
With
sodium tetrahydroborate; sodium hydroxide;
In
isopropyl alcohol;
at 40 ℃;
for 4h;
Cooling with ice;
|
95% |
With
sodium tetrahydroborate;
In
isopropyl alcohol;
at 10 - 55 ℃;
Solvent;
Temperature;
|
94.7% |
With
sodium tetrahydroborate;
In
methanol;
at -10 - 20 ℃;
for 4h;
|
93.2% |
With
methanol; sodium tetrahydroborate;
at -5 - 20 ℃;
for 5h;
|
91.5% |
With
methanol; sodium tetrahydroborate;
In
tetrahydrofuran;
at 20 ℃;
for 1h;
|
|
With
sodium tetrahydroborate;
In
isopropyl alcohol;
at 40 ℃;
for 1h;
|
1.8 g |
7,8-difluoro-6,11-dihydrodibenzo[b,e]thiazepin-11-one
7,8-difluoro-6,11-dihydrodibenzo[b,e]thiazepine-11-ol
Conditions | Yield |
---|---|
With
borane-THF; (S)-5,5-diphenyl-2-methoxy-3,4-propano-1,3,2-oxazaborolidine;
In
toluene;
at 20 - 30 ℃;
for 1.5h;
Reagent/catalyst;
Solvent;
Temperature;
enantioselective reaction;
Inert atmosphere;
|
93.7% |
With
EBSDR8; isopropyl alcohol; NADH;
In
aq. phosphate buffer;
at 30 - 35 ℃;
pH=7.2 - 7.5;
Enzymatic reaction;
|
91% |
With
formic acid; RuCl(p-cymene)[(R,R)-Ts-DPEN]; triethylamine;
In
tetrahydrofuran;
at 60 - 70 ℃;
Inert atmosphere;
|
98.62 % ee |
3,4-Difluorobenzoic acid
3,4-difluoro-2-((phenylthio)methyl)benzoic acid
7,8-difluoro-6,11-dihydrodibenzo[b,e]thiazepin-11-one
sodium thiophenolate
(R)-12-((S)-7,8-difluoro-6,11-dihydrodibenzo[b,e]thiepin-11-yl)-7-hydroxy-3,4,12,12a-tetrahydro-1H-[1,4]oxazino[3,4-c]pyrido[2,1-f][1,2,4]triazine-6,8-dione