Yield:64792-51-4 94%

Reaction Conditions:

with morpholine;sulphur in ethanol at 50;Inert atmosphere;

Steps:

112 Synthesis of compound 112.2.

[00660] Synthesis of compound 112.2. Into a 100-mL 3-necked round-bottom flask under nitrogen were added compound 112.1 (3 g, 23.41 mmol, 1.00 equiv), ethyl 2-cyanoacetate (2.9 g, 25.64 mmol, 1.10 equiv), S (3.0 g) and morpholine (0.75 g) in 50 mL of dry ethanol. The resulting mixture was stirred overnight at 50 °C. Upon completion of the reaction solvent was removed under vacuum and crude was purified via flash column chromatography to afford 5.6 g (94%) of compound 112.2 as a yellow solid.

References:

WO2014/194242,2014,A2 Location in patent:Paragraph 00659-00660