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. 2020 Sep 28;22(10):495–499. doi: 10.1021/acscombsci.0c00173

Table 1. Reaction Conditions for the Three-Component Petasis Reaction Using the Gewald Reaction Product 2a.

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entry solvent time (h) conversion (%)a
1b CH2Cl2 24 24
2b HFIP 1 37
3b MeCN 6 13
4b EtOH 12 trace
5b THF 24 trace
6c CH2Cl2 1 48
7c HFIP 1 63
a

Monitored by LC–MS.

b

Amine 2a and aldehyde 3a were stirred for 10 min before boronic acid 4a was added .

c

Simultaneous addition of all three components.