Back
HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 526938Generated: November 1, 2026

Lithium Hydroxide → N-((trans-2-aminocyclohexyl)methyl)-2-(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)-5-fluoropyrimidin-4-amine

https://huagongshe.com/reaction/526938

Reaction equation

Participants

RoleNameHCIDCharge
ReactantLithium HydroxideHCID 3939—
ReactantN-((trans-2-aminocyclohexyl)methyl)-2-(5-chloro-1-tosyl-1H-pyrrolo[2,3-b]pyridin-3-yl)-5-fluoropyrimidin-4-amineHCID 68007392—
SolventTetrahydrofuranHCID 8028—
SolventEthyl AcetateHCID 8857—
ProductN-((trans-2-aminocyclohexyl)methyl)-2-(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)-5-fluoropyrimidin-4-amineHCID 6800793033%

Reaction Steps

A solution of N-((trans-2-aminocyclohexyl)methyl)-2-(5-chloro-1-tosyl-1H-pyrrolo[2,3-b]pyridin-3-yl)-5-fluoropyrimidin-4-amine, 14f, (0.050 g, 0.077 mmol) in THF was treated with LiOH (0.5 mL, 1.0M) at 60° C. After 5 min, at 120° C., the solution was diluted with EtOAc, and washed with brine, filtered and concentrated in vacuo. Preparative HPLC provided the desired compound, 555, as a racemic mixture of trans isomers (12 mg, 33% yield).

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS09345708B2
Source datasetuspto-grants-2016_05
ORD IDord-c4e3719a1a494e02876edf3b78c721fc
Source noteuspto-grants-2016_05