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. 2023 Jan 24;9(2):e13111. doi: 10.1016/j.heliyon.2023.e13111

Table 6.

Reaction conditions for 1-Phenylcyclopropane carboxamide derivative (8a).

S.No Reagent Base Solvent Time (h) Yield (%)
1 EDC Et3N THF 20 41
2 EDC Et3N DMF 18 45
3 EDC DIPEA THF 16 62
4 EDC DIPEA DMF 12 65
5 HATU Et3N THF 20 46
6 HATU Et3N DMF 18 49
7 HATU DIPEA THF 16 75
8 HATU DIPEA DMF 12 85
9 HBTU Et3N THF 20 48
10 HBTU Et3N DMF 18 51
11 HBTU DIPEA THF 16 68
12 HBTU DIPEA DMF 12 70
13 T3P Et3N THF 20 47
14 T3P Et3N DMF 18 49
15 T3P DIPEA THF 16 64
16 T3P DIPEA DMF 12 68

*All reactions were carried out on a 10 mg scale. The reaction was monitored by TLC and LCMS. Acid (1.0 eq), Amine (1.0 eq), coupling reagent (1.5 eq), base (3.0 eq), solvent (5 vol). EDC (1-Ethyl-3-(3-dimethylaminopropyl)carbodiimide). HATU (1-[Bis(dimethylamino) methylene]-1H-1,2,3-triazolo[4,5-b]pyridinium 3-oxide hexafluoro phosphate). HBTU (3-[Bis(dimethylamino)methyliumyl]-3H-benzotriazol-1-oxide hexafluorophosphate). T3P (Propanephosphonic acid anhydride).