Yield:-

Reaction Conditions:

with N-chloro-succinimide in N,N-dimethyl-formamide at 60; for 1 h;

Steps:

7

To compound 1024 (0.479 mol) in DMF was added NCS (0.5 mol) and the reaction was heated to 60 °C and stirred for one hour to get compound 1025. After cooling the reaction to 0 °C, prop-2-yn-1-ol (0.5 mol) was added. Et3N (0.5 mol) was added to the reaction. The reaction was stirred for another 10 mm. Water and ethyl acetate was added. The aqueous was further extracted with ethyl acetate. The organic layers were washed with brine, dried over sodium sulfate, and concentrate in vacuo. The residue was purified by column chromatography to give compound 1026.

References:

WO2014/18807,2014,A1 Location in patent:Paragraph 00156; 00158