TMSSMe/Cs2CO3 as a methylthiolation reagent

ORGN 121

Qi Qiao, qi.qiao@roche.com, Romyr Dominique, romyr.dominique@roche.com, and Robert Goodnow Jr., robert.goodnow@roche.com. New Lead Chemistry Department, Hoffmann-La Roche Inc, 340 Kingsland St, Nutley, NJ 07110
The combination of (methylthio)trimethylsilane (TMSSMe) and Cs2CO3 in DMSO was found to be efficient as a methylthiolation reagent for electronic withdrawing (EWG) substituted nitrobenzenes. High chemical yields, combined with operationally convenient conditions, render this method practically useful for preparation of thioanisole derivatives.