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. 2024 Feb 7;9(7):7850–7868. doi: 10.1021/acsomega.3c07555

Table 2. Acid Amine Coupling under Different Reaction Conditionsa.

s. no base reagents solvent reaction condition yield (%)
1 TEA EDCI·HCl DCM 32 °C, 12 h 65
2 DMAP DCC DMF 32 °C, 12 h 77
3 DMAP EDCI·HCl CHCl3 32 °C, 12 h, N2 76
4 DMAP EDCI·HCl DCM 32 °C, 12 h, N2 85
5 TEA DCC Benzene 32 °C, 12 h, N2 69
a

All reactions were carried out on a 100 mg scale. Acid (1.0 equiv), amine (1.0 equiv), base (2.0 equiv), reagent (2.0 equiv), and solvent (10 mL). TEA: triethylamine, EDCI·HCl: (3-dimethylamino-propyl)-ethyl-carbodiimide hydrochloride, DMAP: 4 dimethylaminopyridine, DCC: N,N′-dicyclohexylcarbodiimide, h: hour.