Author/Authors :
Bradley O. Ashburn، نويسنده , , Lauren K. Rathbone، نويسنده , , Elizabeth H. Camp، نويسنده , , Rich G. Carter، نويسنده ,
Abstract :
The rapid synthesis of the western biaryl portion of TMC-95 is disclosed via the use of a Diels–Alder reaction with o-nitrostyrene derivative and 1-silyloxy diene with excellent regiochemical control. Subsequent sequential substitutions of a p-iodo-phenol derivative followed by an o-bromo-nitrobenzene intermediate are employed to incorporate the western carbon framework of TMC-95.