Technology Process of 1-((((2S)-4-(2-thiophenylsulfonyl)-1-(4-(2,2,2-trifluoro-1-hydroxy-1-methylethyl)phenyl)-2-piperazinyl)methyl)amino)cyclobutanecarbonitrile
There total 6 articles about 1-((((2S)-4-(2-thiophenylsulfonyl)-1-(4-(2,2,2-trifluoro-1-hydroxy-1-methylethyl)phenyl)-2-piperazinyl)methyl)amino)cyclobutanecarbonitrile which
guide to synthetic route it.
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synthetic route:
- Guidance literature:
-
cyclobutanone; 2-(4-((2S)-2-(aminomethyl)-4-(2-thiophenylsulfonyl)-1-piperazinyl)phenyl)-1,1,1-trifluoro-2-propanol;
In
1,2-dichloro-ethane;
at 20 ℃;
for 0.333333h;
trimethylsilyl cyanide;
In
1,2-dichloro-ethane;
at 20 ℃;
for 12h;
- Guidance literature:
-
Multi-step reaction with 6 steps
1.1: n-butyllithium / diethyl ether; hexanes / 0.25 h / -78 °C
1.2: 0.5 h / -78 °C
2.1: sodium t-butanolate / ruphos; chloro(2-dicyclohexylphosphino-2',6'-di-i-propoxy-1,1'-biphenyl)[2-(2-aminoethylphenyl)]palladium(II) methyl-t-butylether adduct / toluene / 12 h / 65 °C / sealed vessel; Inert atmosphere
3.1: boron trichloride / dichloromethane / 0.67 h / 0 °C
4.1: triethylamine / dichloromethane / 0 °C
5.1: ammonia / methanol / 0.5 h / 140 °C / sealed vial; microwave irradiation
6.1: 1,2-dichloro-ethane / 0.33 h / 20 °C
6.2: 12 h / 20 °C
With
n-butyllithium; ammonia; boron trichloride; triethylamine; sodium t-butanolate;
chloro(2-dicyclohexylphosphino-2',6'-di-i-propoxy-1,1'-biphenyl)[2-(2-aminoethylphenyl)]palladium(II) methyl-t-butylether adduct; ruphos;
In
methanol; hexanes; diethyl ether; dichloromethane; 1,2-dichloro-ethane; toluene;
- Guidance literature:
-
Multi-step reaction with 5 steps
1.1: sodium t-butanolate / ruphos; chloro(2-dicyclohexylphosphino-2',6'-di-i-propoxy-1,1'-biphenyl)[2-(2-aminoethylphenyl)]palladium(II) methyl-t-butylether adduct / toluene / 12 h / 65 °C / sealed vessel; Inert atmosphere
2.1: boron trichloride / dichloromethane / 0.67 h / 0 °C
3.1: triethylamine / dichloromethane / 0 °C
4.1: ammonia / methanol / 0.5 h / 140 °C / sealed vial; microwave irradiation
5.1: 1,2-dichloro-ethane / 0.33 h / 20 °C
5.2: 12 h / 20 °C
With
ammonia; boron trichloride; triethylamine; sodium t-butanolate;
chloro(2-dicyclohexylphosphino-2',6'-di-i-propoxy-1,1'-biphenyl)[2-(2-aminoethylphenyl)]palladium(II) methyl-t-butylether adduct; ruphos;
In
methanol; dichloromethane; 1,2-dichloro-ethane; toluene;