Table 2: Coupling conditions and isolated yield for 5ae and 7ae.

Entry Starting materialReagents/conditionsProduct (isolated yield%)α : β
ratio

14aHA1.3 eq. EDC, cat. DMAP, r.t., 12 h720 : 112.5
24bHA1.3 eq. EDC, cat. DMAP, r.t., 12 h690 : 113.3
34cHA1.3 eq. EDC, cat. DMAP, r.t., 12 h650 : 127.1
44dHA1.3 eq. EDC, cat. DMAP, r.t., 12 h670 : 143.3
54eHA1.3 eq. EDC, cat. DMAP, r.t., 12 h680 : 147.1
66aHA1.3 eq. EDC, cat. DMAP, r.t., 18 h721 : 326.5
76bHA1.3 eq. EDC, cat. DMAP, r.t., 18 h741 : 321.6
86cHA1.3 eq. EDC, cat. DMAP, r.t., 18 h701 : 117.3
96dHA1.3 eq. EDC, cat. DMAP, r.t., 18 h671 : 345.0
106eHA1.3 eq. EDC, cat. DMAP, r.t., 18 h631 : 333.3

= 24 mg/2 mL in dichloromethane.