Updated reaction protocols in microwave-assisted SPPS
Strategy | Reagents and conditions | Ref. |
---|---|---|
Boc | Solvent: DMF Deprotection: 100% TFA Coupling: HOBt, DIC, and DIPEA or HBTU and DIPEA (for Boc-Asn) | [177] |
Fmoc | Solvent: DMF Deprotection: 10% (w/v) piperazine or 20% (v/v) piperidine Coupling: Oxyma pure and DIC | [178, 179] |
Fmoc | Solvent: DMF Deprotection: 10% (w/v) piperazine or 20% (v/v) piperidine Coupling: HOBt and DIC or HBTU (or HATU) and DIPEA | [171, 180–183] |
Fmoc | Solvent: NMP Deprotection: 10% (w/v) piperazine or 20% (v/v) piperidine Coupling: HBTU (or HATU) and DIPEA | [184] |
Ref.: reference; DMF: dimethylformammide; TFA: trifuoloacetic acid; HOBt: hydroxybenzotriazole; DIC: N,N-Diisopropylcarbodiimide; DIPEA: N,N-Diisopropynethylamine; HBTU: 2-(1H-Benzotriazole-1-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate; NMP: N-Methyl-2-pyrrolidone; HATU: 1-[Bis(dimethylamino)methylene]-1H-1,2,3-triazolo[4,5-b]pyridinium 3-oxid hexafluorophosphate