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. 2016 May 27;7(8):785–790. doi: 10.1021/acsmedchemlett.6b00186

Scheme 3. Alkylation of 17a and 17b To Give Analogues 18a18c and Conversion of Isocyanate 19 To Give Thioethers 20a/b.

Scheme 3

Reagents and conditions: (a) 2-chloroacetyl chloride, Et3N, CH2Cl2, rt, overnight, 99%; (b) chloromethanesulfonyl chloride, Et3N, CH2Cl2, rt, overnight, 85%; (c) NaH, THF, rt, 1–2 d, 4–99%; (d) DPPA, Et3N, toluene, reflux, overnight, 17–65%.