Technology Process of N-{3-[(4aS,5S,7aS)-2-amino-5-(trifluoromethyl)-4a,5-dihydro-4H-furo[3,4-d][1,3]thiazin-7a(7H)-yl]-4-fluorophenyl}-5-[(2H3)methyloxy]pyrazine-2-carboxamide
There total 20 articles about N-{3-[(4aS,5S,7aS)-2-amino-5-(trifluoromethyl)-4a,5-dihydro-4H-furo[3,4-d][1,3]thiazin-7a(7H)-yl]-4-fluorophenyl}-5-[(2H3)methyloxy]pyrazine-2-carboxamide which
guide to synthetic route it.
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synthetic route:
- Guidance literature:
-
C24H22(2)H3F4N5O5S;
With
trifluoroacetic acid;
In
dichloromethane;
at 20 ℃;
for 2h;
With
sodium hydrogencarbonate;
In
water;
Saturated solution;
- Guidance literature:
-
Multi-step reaction with 11 steps
1.1: hydroxylamine hydrochloride; sodium acetate / methanol / 1.5 h / 50 °C
2.1: hydroquinone / xylene / 22 h / Reflux
3.1: zinc; acetic acid / 0 - 20 °C
4.1: dichloromethane / 18 h / 20 °C
5.1: trifluoromethylsulfonic anhydride; pyridine / -20 - 0 °C
6.1: 1,8-diazabicyclo[5.4.0]undec-7-ene; methanol / 16 h / Reflux
7.1: nitric acid; trifluoroacetic acid; sulfuric acid / 1.83 h / 0 °C
7.2: pH 12 / Cooling with ice
8.1: tetrahydrofuran / 60 °C
9.1: ethanol; tin(II) chloride dihdyrate / 18 h / 20 °C
10.1: N-ethyl-N,N-diisopropylamine; benzotriazol-1-yloxyl-tris-(pyrrolidino)-phosphonium hexafluorophosphate / dichloromethane / 18 h / 20 °C
11.1: trifluoroacetic acid / dichloromethane / 2 h / 20 °C
11.2: Saturated solution
With
pyridine; methanol; tin(II) chloride dihdyrate; ethanol; trifluoromethylsulfonic anhydride; sulfuric acid; hydroxylamine hydrochloride; benzotriazol-1-yloxyl-tris-(pyrrolidino)-phosphonium hexafluorophosphate; nitric acid; sodium acetate; acetic acid; 1,8-diazabicyclo[5.4.0]undec-7-ene; N-ethyl-N,N-diisopropylamine; hydroquinone; trifluoroacetic acid; zinc;
In
tetrahydrofuran; methanol; dichloromethane; xylene;
- Guidance literature:
-
Multi-step reaction with 6 steps
1.1: 1,8-diazabicyclo[5.4.0]undec-7-ene; methanol / 16 h / Reflux
2.1: nitric acid; trifluoroacetic acid; sulfuric acid / 1.83 h / 0 °C
2.2: pH 12 / Cooling with ice
3.1: tetrahydrofuran / 60 °C
4.1: ethanol; tin(II) chloride dihdyrate / 18 h / 20 °C
5.1: N-ethyl-N,N-diisopropylamine; benzotriazol-1-yloxyl-tris-(pyrrolidino)-phosphonium hexafluorophosphate / dichloromethane / 18 h / 20 °C
6.1: trifluoroacetic acid / dichloromethane / 2 h / 20 °C
6.2: Saturated solution
With
methanol; tin(II) chloride dihdyrate; ethanol; sulfuric acid; benzotriazol-1-yloxyl-tris-(pyrrolidino)-phosphonium hexafluorophosphate; nitric acid; 1,8-diazabicyclo[5.4.0]undec-7-ene; N-ethyl-N,N-diisopropylamine; trifluoroacetic acid;
In
tetrahydrofuran; dichloromethane;
