تفاعل #1932351

معادلة التفاعل

5-(isobutyl(methyl)carbamoyl)-4′-methylbiphenyl-3-carboxylic acid

N-(3-dimethylaminopropyl)-N′-ethylcarbodiimide hydrochloride

1-hydroxybenzotriazole hydrate

(R)-1-(2-methylpyrimidin-5-yl)ethanamine

N,N-diisopropylethylamine

→

(R)—N3-Isobutyl-N3,4′-dimethyl-N5-(1-(2-methylpyrimidin-5-yl)ethyl)biphenyl-3,5-dicarboxamide

المذيبات

CH2Cl2

ظروف التفاعل

المعالجة

1. 1
   تركيزconcentrated in vacuo
2. 2
   أخرىThe residue was purified by preparative HPLC (100×21.2 mm C18 column, 40-70% MeCN/water[10 mM Et2NH])
3. 3
   أخرىto afford a white foam

الإجراء التجريبي

To a mixture of 5-(isobutyl(methyl)carbamoyl)-4′-methylbiphenyl-3-carboxylic acid (15 mg, 0.046 mmol), N-(3-dimethylaminopropyl)-N′-ethylcarbodiimide hydrochloride (18 mg, 0.092 mmol), 1-hydroxybenzotriazole hydrate (7.0 mg, 0.046 mmol), and CH2Cl2 (2 mL) were added (R)-1-(2-methylpyrimidin-5-yl)ethanamine (9.5 mg, 0.069 mmol) (WO 2008/130481) and N,N-diisopropylethylamine (12 μL, 0.069 mmol). The mixture was stirred at room temperature overnight, and then concentrated in vacuo. The residue was purified by preparative HPLC (100×21.2 mm C18 column, 40-70% MeCN/water[10 mM Et2NH]) to afford a white foam.

المصدر