The asymmetric synthesis of the HIV non-nucleoside reverse transcriptase inhibitor (NNRTI) DPC 961 is achieved in three steps with an overall yield of> 55%. The asymmetry is induced by the chiral auxiliary (R)-(+)-α-methylbenzylamine, utilizing a new asymmetric 1, 4-addition protocol.
[Magnus, Nicholas A.; Confalone, Pat N.; Storace, Louis; Patel, Mona; Wood, Christopher C.; Davis, Wayne P.; Parsons Jr., Rodney L. Journal of Organic Chemistry, 2003 , vol. 68, # 3 p. 754 - 761]
[Magnus, Nicholas A.; Confalone, Pat N.; Storace, Louis; Patel, Mona; Wood, Christopher C.; Davis, Wayne P.; Parsons Jr., Rodney L. Journal of Organic Chemistry, 2003 , vol. 68, # 3 p. 754 - 761]