Table 2 Scope of enoldiazoacetates: effect of the carboxylate group.

From: Chiral donor–acceptor azetines as powerful reactants for synthesis of amino acid derivatives

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Entrya

R1

R2

Yield 3 (%)b

ee (%)c

1

Et

iPr

3g 82

89

2

Et

Bn

3h 87

92

3

Et

4-BrBn

3i 90

90

4

Et

4-OMeBn

3j 95

99

5d

Et

3,4,5-triOMeBn

3k 70

98

6

Et

4-CF3Bn

3l 73

87

7

Me

4-OMeBn

3m 77

88

  1. aAll reactions were carried out on a 0.20 mmol scale in 4.0 mL DCM: 2a (0.20 mmol), 1a (0.24 mmol)
  2. bIsolated yield after flash chromatography
  3. cDetermined by chiral HPLC analysis
  4. dReaction time was 48 h