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. 2017 May 31;13:1050–1063. doi: 10.3762/bjoc.13.104

Table 1.

CBB-3CR involving tert-butylisocyanide.

graphic file with name Beilstein_J_Org_Chem-13-1050-i001.jpg

Entry Starting materials Method Product Yield, %
Aldehydes R1 Aminopyrazoles R2

1 1a H 2a 4-F A 4a 54
2 1b 2-CH3O 2a 4-F A 4b 75
3 1c 3-CH3O 2a 4-F A 4c 77
4 1d 4-CH3O 2a 4-F A 4d 75
5 1e 4-Cl 2a 4-F A 4e 72
6 1b 2-CH3O 2b 3-F A 4f 83
7 1d 4-CH3O 2b 3-F A 4g 64
8 1e 4-Cl 2b 3-F A 4h 89
9 1b 2-CH3O 2c 2-CH2CH3 A 4i 82
10 1d 4-CH3O 2c 2-CH2CH3 A 4j 64
11 1e 4-Cl 2c 2-CH2CH3 A 4k 66
12 1b 2-CH3O 2d 4-CH2CH3 A 4l 85
13 1e 4-Cl 2d 4-CH2CH3 A 4m 53
14 1f 4-CO2CH3 2a 4-F B 4n 85
15 1g 4-NO2 2a 4-F B 4o 87
16 1h 4-CN 2a 4-F B 4p 90
17 1f 4-CO2CH3 2b 3-F B 4q 88
18 1g 4-NO2 2b 3-F B 4r 87
19 1h 4-CN 2b 3-F B 4s 82
20 1f 4-CO2CH3 2c 2-CH2CH3 B 4t 61
21 1g 4-NO2 2c 2-CH2CH3 B 4u 79
22 1h 4-CN 2c 2-CH2CH3 B 4v 83