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. 2020 Nov 3;26(69):16241–16245. doi: 10.1002/chem.202002449

Scheme 7.

Scheme 7

Late stage modification of 9. a) HCl, acetone, r.t., 2.5 h, 66 %; b) Grubbs II catalyst (20 mol %), toluene, 80 °C, 18 h, 69 % brsm; c) HCl, acetone, r.t., 3 h, 78 %; d) potassium thioacetate, acetone, r.t., 3 h, 78 %; e) HCl, acetone, r.t., 3 h, 61 %; f) Grubbs II catalyst (20 mol %), toluene, 80 °C, 18 h, 52 % brsm; g) HCl, acetone, r.t., 2.5 h, 58 %; h) TFA, Et3SiH, DCM, r.t., 5 min.