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. 2020 Jun 22;15(14):1294–1309. doi: 10.1002/cmdc.202000250

Table 1.

Yields and melting points of amides (3) when using the B(OCH3)3 amidation method.

Cmpd

R1

R2

Yield [%]

Mp [°C]

3 a

H

H

98

108–110

3 b

4‐F

H

89

114–116

3 c

4‐Cl

H

85

135–136

3 d

4‐Cl

Cl

84

126–128

3 e

2,4‐diCl

H

100

78–80

3 f

2,4‐diCl

Cl

40

106–108

3 g

4‐CH3

H

100

96–98

3 h

4‐CF3

H

34

104–106

3 i

4‐OCH3

H

98

126–128

3 j

3,4‐diOCH3

H

83

116–118

3 k

NHBoc

H

79

118–120