反应详情

Rac-cis-cyclopentane-1,2-dicarboxylic acid monomethyl ester (172 mg) was dissolved in DMF (5 mL) and treated with HATU (1.1 eq. 470 mg) and DIEA (3 eq, 500 μL) and stirred for 15 minutes. Then 4-(2-amino-thiazol-4-yl)-N-cyclopropyl-benzamide (1 eq, 260 mg) was added and the mixture stirred at ambient temperature overnight. The reaction was cooled, filtered and the solvents removed. The resulting mixture was redissolved in 5 ml of 90% DMF, 10% water with 0.1% TFA and purified by reverse phase HPLC to give the product. MS: 414.5.

1. stirringthe mixture stirred at ambient temperature overnight
2. temperatureThe reaction was cooled
3. filtrationfiltered
4. customthe solvents removed
5. dissolutionThe resulting mixture was redissolved in 5 ml of 90% DMF
6. custom10% water with 0.1% TFA and purified by reverse phase HPLC
7. customto give the product