Process development and multikilogram syntheses of XL228 utilizing a regioselective isoxazole formation and a selective SNAr reaction to a pyrimidine core

NR Guz, H Leuser, E Goldman

Index: Kumar, C.H. Vinod; Kavitake, Santosh; Kumar, Sythana Suresh; Cornwall, Philip; Ashok, Mithun; Bhagat, Sagar; Manjunatha, Sulur G.; Nambiar, Sudhir Organic Process Research and Development, 2012 , vol. 16, # 8 p. 1416 - 1421

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Citation Number: 5

Abstract

... Organic Process Research & Development. ... C, 24 h, 98% conversion by LC; (c) 9, DMA, 30 °C, 10 h, 87% conversion by LC; (d) 3, DMA, 30 °C, 12 h, 97% conversion by LC; (e) CH 3 CN ... (f) iPrOAc, H 2 O, K 2 CO 3 , 20 °C, then 7, iPrOAc, reflux, 4 h, 99% conversion by LC; (g) K 2 ...