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. 2020 Mar 11;26(19):4289–4296. doi: 10.1002/chem.201904073

Table 1.

Preparation of diamides 3944 (COMU = 1‐cyano‐2‐ethoxy‐2‐oxoethylideneaminooxy) dimethylamino‐morpholino‐carbenium‐hexafluorophosphate).

graphic file with name CHEM-26-4289-g009.jpg

Building block ring A

Building block ring B

Conditions

Yields [%]

33

7

Na2CO3, THF, H2O, rt, 3 h

39 (98)

34

32

for 3438:

COMU, DIPEA, DMF, rt, 16 h, then TFA, rt, 30 min

40 (75)

35

32

41 (66)

36

32

42 (94)

37

32

43 (83)

38

32

44 (79)