تفاعل #325171

معادلة التفاعل

Na2CO3

(4-Cyanomethylphenyl)boronic acid

3-iodo-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-4-amine

→

2-(4-(4-amino-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)phenyl)acetonitrile

المذيبات

EtOH

DME

ظروف التفاعل

المعالجة

1. 1
   درجة الحرارةAfter cooling
2. 2
   استخلاصthe reaction was extracted with saturated NaCl and CH2Cl2
3. 3
   تركيزconcentrated in vacuo
4. 4
   أخرىpurified by RP-HPLC (MeCN:H2O:0.1% TFA)
5. 5
   أخرىto yield BA45

الإجراء التجريبي

A solution of (4-Cyanomethylphenyl)boronic acid (18 mg, 0.11 mmol) in EtOH (3.3 ml) was added to a solution of 3-iodo-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-4-amine (30 mg, 0.10 mmol) in DME (12 ml). Pd(PPh3)4 (30 mg, 0.03 mmol) and saturated Na2CO3 (1.9 ml) were added and the reaction was heated to 80° C. under an argon atmosphere overnight. After cooling, the reaction was extracted with saturated NaCl and CH2Cl2. Organic phases were combined, concentrated in vacuo and purified by RP-HPLC (MeCN:H2O:0.1% TFA) to yield BA45. ESI-MS (M+H)+ m/z calcd 293.1, found 293.1.

المصدر