4-Amino-1-Boc-piperidine → HCID 178452100, compound

Participants

Reaction Steps

A suspension of benzyl (3,5-diamino-6-chloropyrazine-2-carboxamido)(methylthio)methylenecarbamate (Intermediate B) (6.7 g, 17 mmol) and 4-amino-1-Boc-piperidine (4.1 g, 20.4 mmol) in dry THF (150 mL) is heated at reflux overnight. The solvent is removed in vacuo and a solid forms on concentration. The solid is separated and retained and the remaining mother liquor is concentrated to form a solid. The solid is partitioned between EtOAc and water and the organic portion is dried (MgSO4) and part concentrated in vacuo and then left to crystallise. The crystals are filtered and combined with the retained solid to afford the title product. [M+H]+ 547

Provenance & Evidence