تفاعل #45227

معادلة التفاعل

NaOH

HCl

solution

2-[3-(3-tert-butyl-5-amino-1H-pyrazol-1-yl)phenyl]acetamide

borane methylsulfide

→

3-tert-butyl-1-[3-(2-aminoethyl)phenyl]-1H-pyrazol-5 amine

المردود 47.4%

المذيبات

THF

ظروف التفاعل

المعالجة

1. 1
   درجة الحرارةThe mixture was heated
2. 2
   درجة الحرارةto reflux for 90 min
3. 3
   درجة الحرارةheated
4. 4
   درجة الحرارةto reflux for 10 min
5. 5
   استخلاصextracted with EtOAc
6. 6
   تجفيفThe organic layer was dried (Na2SO4)
7. 7
   ترشيحfiltered
8. 8
   تركيزconcentrated in vacuo

الإجراء التجريبي

To a stirred solution of Example N (2 g, 7.35 mmol) in THF (6 ml) was added borane-methylsulfide (18 mmol). The mixture was heated to reflux for 90 min and cooled to RT, after which 6 N HCl was added and heated to reflux for 10 min. The mixture was basified with NaOH and extracted with EtOAc. The organic layer was dried (Na2SO4) filtered and concentrated in vacuo to yield 3-tert-butyl-1-[3-(2-aminoethyl)phenyl]-1H-pyrazol-5 amine (0.9 g).

المصدر