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. 2009 Aug 26;131(37):13255–13269. doi: 10.1021/ja809933h

Scheme 2. Simplified Strategy for cMO Synthesis.

Scheme 2

Reagents and conditions: (a) 2,5-dioxopyrrolidin-1-yl 3-azidopropanoate, 0.1 M sodium borate (pH 8.5)/3:1 (v/v) DMSO, 98%; (b) bifunctional DMNB linker 2a or 2b, 0.1 M sodium borate (pH 8.5)/DMSO 6:1 (v/v), 70−90%; (c) sodium ascorbate, TBTA, CuI, 0.1 M potassium phosphate (pH 8.0), DMSO, 10−25% after HPLC. The ntla cMOs 8a−h, 8a′, and 8e′ were prepared through this synthetic route, using the ntla-targeting MO (5′-GACTTGAGGCAGACATATTTCCGAT-5′) and inhibitory MOs having various lengths and sequences (Table 1).