Technology Process of (4aS,5S,7aS)-7a-(5-amino-2,3-difluorophenyl)-5-(fluoromethyl)-4a,5,7,7a-tetrahydro-4H-furo[3,4-d][1,3]thiazin-2-amine
There total 18 articles about (4aS,5S,7aS)-7a-(5-amino-2,3-difluorophenyl)-5-(fluoromethyl)-4a,5,7,7a-tetrahydro-4H-furo[3,4-d][1,3]thiazin-2-amine which
guide to synthetic route it.
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synthetic route:
- Guidance literature:
-
(4aS,5S,7aS)-7a-(2,3-difluoro-5-nitrophenyl)-5-(fluoromethyl)-4a,5,7,7a-tetrahydro-4H-furo[3,4-d][1,3]thiazin-2-amine;
With
hydrogenchloride; iron; ammonium chloride;
In
ethanol; water;
at 55 ℃;
for 0.5h;
With
sodium hydroxide;
In
water;
- Guidance literature:
-
Multi-step reaction with 6 steps
1: trifluoromethylsulfonic anhydride; pyridine / dichloromethane / 1.5 h / 0 °C
2: hydrogenchloride; water / methanol
3: Nonafluorobutanesulfonyl fluoride; N-ethyl-N,N-diisopropylamine; triethylamine tris(hydrogen fluoride) / tetrahydrofuran / 0 - 20 °C / Inert atmosphere
4: 1,8-diazabicyclo[5.4.0]undec-7-ene; methanol / 8 h / 55 - 60 °C / Inert atmosphere
5: nitric acid; trifluoroacetic acid; sulfuric acid / 0 - 5 °C
6: hydrogenchloride; ammonium chloride; iron / ethanol; water / 0.5 h / 55 °C
With
pyridine; hydrogenchloride; methanol; Nonafluorobutanesulfonyl fluoride; trifluoromethylsulfonic anhydride; sulfuric acid; water; nitric acid; iron; ammonium chloride; 1,8-diazabicyclo[5.4.0]undec-7-ene; triethylamine tris(hydrogen fluoride); N-ethyl-N,N-diisopropylamine; trifluoroacetic acid;
In
tetrahydrofuran; methanol; ethanol; dichloromethane; water;
- Guidance literature:
-
Multi-step reaction with 4 steps
1: Nonafluorobutanesulfonyl fluoride; N-ethyl-N,N-diisopropylamine; triethylamine tris(hydrogen fluoride) / tetrahydrofuran / 0 - 20 °C / Inert atmosphere
2: 1,8-diazabicyclo[5.4.0]undec-7-ene; methanol / 8 h / 55 - 60 °C / Inert atmosphere
3: nitric acid; trifluoroacetic acid; sulfuric acid / 0 - 5 °C
4: hydrogenchloride; ammonium chloride; iron / ethanol; water / 0.5 h / 55 °C
With
hydrogenchloride; methanol; Nonafluorobutanesulfonyl fluoride; sulfuric acid; nitric acid; iron; ammonium chloride; 1,8-diazabicyclo[5.4.0]undec-7-ene; triethylamine tris(hydrogen fluoride); N-ethyl-N,N-diisopropylamine; trifluoroacetic acid;
In
tetrahydrofuran; ethanol; water;