Scheme 1–

Synthesis of Thalidomide and screening of reaction conditions.

Entry	Solvent	Temperature / °C	Isolated Yield
1	Trifluoroethanol	150	91%(a)
2	Ethanol	150	24%(a)
3	10% TFA in Ethanol	150	Complex Mixture(a)
4	Trifluoroethanol	Reflux	No Reaction(b)
5	Trifluoroethanol	150	72%(c)
6	Trifluoroethanol	150	62%(a)(d)

^[a]heated under microwave conditions

^[b]heated in an oil bath

^[c]heated in an oil bath at 150° in a seal tube

^[d]phthalic acid used in place of phthalic anhydride