Figures & data
Scheme 1. Reagents and conditions: (1) MePPh3Br, tBuOK, THF, rt, 18 h; (2) NEt3, CH2Cl2, 0 °C to rt, 18 h; (3) 5 (CAS: 250220–36-1), PhMe, 70 °C, 4 h; (iv) TMSBr, CH2Cl2, rt, 24 h.
![Scheme 1. Reagents and conditions: (1) MePPh3Br, tBuOK, THF, rt, 18 h; (2) NEt3, CH2Cl2, 0 °C to rt, 18 h; (3) 5 (CAS: 250220–36-1), PhMe, 70 °C, 4 h; (iv) TMSBr, CH2Cl2, rt, 24 h.](/cms/asset/ff95c88b-31be-4a42-89fc-d782a838bb7e/ienz_a_2249267_sch0001_c.jpg)
Scheme 2. Reagents and conditions: (1) Pd(dppf)Cl2, K2CO3, 1,4-dioxane/H2O (5:1), 80 °C, 16 h, 54–63%.
![Scheme 2. Reagents and conditions: (1) Pd(dppf)Cl2, K2CO3, 1,4-dioxane/H2O (5:1), 80 °C, 16 h, 54–63%.](/cms/asset/df726afe-2f2e-4062-bd18-c075fdd17366/ienz_a_2249267_sch0002_c.jpg)
Scheme 3. Reagents and conditions: (1) Pd(dppf)Cl2, K2CO3, 1,4-dioxane/H2O (5:1), 80 °C, 16 h, 57–69%.
![Scheme 3. Reagents and conditions: (1) Pd(dppf)Cl2, K2CO3, 1,4-dioxane/H2O (5:1), 80 °C, 16 h, 57–69%.](/cms/asset/2bb522aa-0835-4083-94f0-0d72d7c09f0e/ienz_a_2249267_sch0003_c.jpg)
Scheme 4. Reagents and conditions: (1) Pd(dppf)Cl2, K2CO3, 1,4-dioxane/H2O (5:1), 80 °C, 16 h, 66–89%.
![Scheme 4. Reagents and conditions: (1) Pd(dppf)Cl2, K2CO3, 1,4-dioxane/H2O (5:1), 80 °C, 16 h, 66–89%.](/cms/asset/cbcbff69-1d84-420d-bdfa-6813be04665d/ienz_a_2249267_sch0004_c.jpg)
Table 1. Inhibition data of compounds 7–10 and the standard inhibitor acetazolamide (AAZ) against human CA isoforms I, II, IX and XII by the stopped-flow CO2 hydrase assay.
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