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