MeOH |
DMT-MM, 80 ℃, 1 hour |
Methylester/ Lactone |
— |
— |
Wheeler et al., 200948)
|
|
|
Ammonia |
DMT-MM, 60 ℃, 15 hours |
Amide/ Lactone |
Solid-phase permethylation, room temp., 0.5 hour |
Over 15 hours |
Alley et al., 201049)
|
|
|
EtOH |
EDC+HOBt, 37 ℃, 1∼2 hours |
Ethylester/ Lactone |
— |
— |
Reiding et al., 201450)
|
|
|
|
|
Lactone cleavage (pH 10, 1 hour) followed by methylamidation by PyAOP (room temp., 0.5 hour) |
2.5 hours |
Li et al., 201654)
|
STSD |
Amidation by p-toluidine, room temp., 3 hours |
5 hours |
Yang et al., 201757)
|
|
Amidation by ethylenediamine (EDA), 37 ℃, 3 hours |
5 hours |
Yang et al., 201858)
|
Amidation by EDC+HOBt, 60 ℃, 2 hours |
3 hours |
Lageveen-Kammeijer and de Haan et al., 201960)
|
|
Dimethylamine |
EDC+HOBt in DMSO, 60 ℃, 1∼3 hours |
Dimethylamide/ Lactone |
— |
— |
de Haan et al., 201551)
|
|
|
|
|
Amidation by EDC+HOBt, 60 ℃, 2 hours |
3 hours |
Holst et al., 201655)
|
Double amidation |
Permethylation |
2.5 hours |
Jiang et al., 201756)
|
SSAP |
|
Isopropylamine |
EDC+HOBt in DMSO, room temp., 1∼2 hours |
Isopropylamide/ Lactone |
Methylamidation by PyAOP, room temp., 1 hour |
2 hours |
Nishikaze et al., 201752)
|
SALSA |
|
|
|
Aminolysis by methylamine or ethylamine, room temp., Few seconds |
1 hour |
Hanamatsu et al., 201859)
|
Aminolysis-SALSA |
Methylamidation by EDC+ HOBt, 60 ℃, 2 hours |
4 hours |
Suzuki et al., 201869)
|
Modified-SALSA |