ethyl 1-(methylsulfonyl)cyclopropanecarboxylate synthesis

Yield:1257236-76-2 78%

Reaction Conditions:

with potassium carbonate in N,N-dimethyl-formamide at 60; for 24 h;

Steps:

O.b

To a solution of compound ethyl 2-methylsulfonylacetate (01 , 166 g, 1.0 mol ) in DMF (1500 ml.) was added 1 ,2-dibromoethane (265 g, 1.4 mol) and K₂CO₃ (207 g, 1.5 mol). The reaction mixture was stirred at 60⁰C for 24 hours. Water and ethyl acetate was added while stirring, the separated organic layer was washed with brine, dried over Na₂SO₄, and concentrated in vacuo to give ethyl 1-methylsulfonylcyclopropane-i-carboxylate (150 g, 78%); ¹H NMR (400 MHz, CDCI₃) δ 4.27 (2H, q, CH₂), 3.15 (3H, s, CH₃), 1.80 (2H, m, CH₂), 1.65 (2H, m, CH₂), 1.31 (3H, t, CH₃).

References:

WO2010/136778,2010,A1 Location in patent:Page/Page column 61