Table 1 Scope of enoldiazoacetates: effect of the R-substituent.

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

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Entrya

R

Yield 3 (%)b

ee (%)c

1

Me

3b 82

75

2

Et

3c 92

90

3d

Bn

3d 73

90

4d

iPr

3e 70

92

5d

n-C8H17

3f 63

97

  1. aAll reactions were carried out on a 0.20 -mmol scale in 4.0 mL of 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 72 h
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