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. Author manuscript; available in PMC: 2019 Apr 6.
Published in final edited form as: J Org Chem. 2018 Mar 13;83(7):3417–3425. doi: 10.1021/acs.joc.7b03100

Table 3.

Substrate scope of azaheterocycle N-cyclopropylation.a

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a

All reactions were run on a 0.3–0.6 mmol scale. Percentages correspond to isolated yields.

b

13% of the mono-cyclopropylated product (8a′) was also isolated.

c

With 10% Cu(OAc)2 and 10% phen under otherwise identical conditions: 49% 8a (bis), 15% 8a′ (mono). The connectivity of 8a′ was confirmed by single-crystal X-ray diffraction (see SI).

d

25 mol% Cu(OAc)2, 25 mol% phen.