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. Author manuscript; available in PMC: 2023 Aug 11.
Published in final edited form as: J Med Chem. 2022 Jul 26;65(15):10251–10284. doi: 10.1021/acs.jmedchem.2c00552

Scheme 6.

Scheme 6.

Preparation and derivatization of the bromo regioisomers 27 and 28.

Reagents and conditions. a. diethyl oxalate, reflux; b. SOCl2, DMF cat.; c. Malononitrile, NaH, DME; d. 92, NMP; e. H2SO4; f. BBr3, CH2Cl2; g. RB(OR)2, Pd(dppf)Cl2.CH2Cl2, K2CO3, DMF or CuCN, DMF.