Technology Process of 5-[3-[4-(4-fluorophenyl)piperazin-1-yl]propyl]-2-methyl-2,4,5,6,7,8-hexahydropyrrolo[3,4-c]azepine-4,8-dione
There total 6 articles about 5-[3-[4-(4-fluorophenyl)piperazin-1-yl]propyl]-2-methyl-2,4,5,6,7,8-hexahydropyrrolo[3,4-c]azepine-4,8-dione which
guide to synthetic route it.
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synthetic route:
- Guidance literature:
-
With
potassium carbonate; sodium iodide;
In
acetonitrile;
for 38h;
Heating;
DOI:10.1248/cpb.48.623
- Guidance literature:
-
Multi-step reaction with 4 steps
1: 87 percent / 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride; 4-dimethylaminopyridine; Et3N / CH2Cl2 / 5 h / 20 °C
2: 2 N aq. NaOH / tetrahydrofuran / 0.5 h / 20 °C
3: 8.4 percent / P2O5; CH3SO3H / 0.5 h / 90 °C
4: 93 percent / K2CO3; NaI / acetonitrile / 38 h / Heating
With
dmap; sodium hydroxide; methanesulfonic acid; phosphorus pentoxide; potassium carbonate; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; triethylamine; sodium iodide;
In
tetrahydrofuran; dichloromethane; acetonitrile;
1: Acylation / 2: Hydrolysis / 3: Cyclization / 4: Alkylation;
DOI:10.1248/cpb.48.623
- Guidance literature:
-
Multi-step reaction with 6 steps
1.1: t-BuOK; 18-crown-6 / diethyl ether / 0 °C
1.2: 78 percent / diethyl ether / 1 h / 20 °C
2.1: 79 percent / 1 N aq. NaOH / methanol / 6 h / Heating
3.1: 87 percent / 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride; 4-dimethylaminopyridine; Et3N / CH2Cl2 / 5 h / 20 °C
4.1: 2 N aq. NaOH / tetrahydrofuran / 0.5 h / 20 °C
5.1: 8.4 percent / P2O5; CH3SO3H / 0.5 h / 90 °C
6.1: 93 percent / K2CO3; NaI / acetonitrile / 38 h / Heating
With
dmap; sodium hydroxide; methanesulfonic acid; 18-crown-6 ether; potassium tert-butylate; phosphorus pentoxide; potassium carbonate; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; triethylamine; sodium iodide;
In
tetrahydrofuran; methanol; diethyl ether; dichloromethane; acetonitrile;
1.1: Metallation / 2.1: Hydrolysis / 3.1: Acylation / 4.1: Hydrolysis / 5.1: Cyclization / 6.1: Alkylation;
DOI:10.1248/cpb.48.623