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. Author manuscript; available in PMC: 2015 Nov 13.
Published in final edited form as: J Med Chem. 2013 Aug 2;56(16):6434–6456. doi: 10.1021/jm400652r

Scheme 1. Synthesis of dihydro-quinolone-pyrazoline derivatives.

Scheme 1

(a) Anhydrous THF, Triphosgene (warning, triphosgene is toxic, see Methods), reflux. (b) EtOH, Weinreb’s HCl salt, reflux. (c) Anhydrous THF, n-Butyllithium, −78 °C. (d) Ethylacetoacetate, DMF, 4Å molecular sieves, 180 °C, µW. (e) 4:3 EtOH:H2O (0.05 M), 0 °C to r.t. (f) hydrazine monohydrate, EtOH, 110 °C, µW. (g) Anhydrous THF, 4Å molecular sieves, 165 °C, µW.