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. 2023 Feb 16;16(2):310. doi: 10.3390/ph16020310

Table 1.

General conditions for the synthesis of the series 1 (compounds 1122).

Compound X5 Isocyanide Acid Time (h) Yield (%) a,b,c
11 H tert-butyl ClCH2COOH 48 65
12 I tert-butyl ClCH2COOH 72 28
13 NO2 tert-butyl ClCH2COOH 72 52
14 Cl (Cl = X7) tert-butyl ClCH2COOH 72 30
15 Br Cyclohexyl CF3COOH 48 58
16 Br tert-butyl ClCH2COOH 72 21
17 I tert-butyl CF3COOH 48 60
18 I Cyclohexyl CF3COOH 48 55
19 Br tert-butyl CF3COOH 48 58
20 NO2 tert-butyl CF3COOH 48 55
21 NO2 Cyclohexyl CF3COOH 48 57
22 Br Cyclohexyl ClCH2COOH 72 42

a Yield after purification. b All reactions used n-butylamine as the amino component, molecular sieves 3Å, rt. c All reactions were treated with Capsule@Amberlyst-15 for isocyanide scavenging.