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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1923330Generated: October 27, 2026

Trifluoroacetic acid → 3-[2-(2-Ethylbenzoimidazol-1-yl)-9-methyl-6-morpholin-4-yl-9H-purin-8-yl]azetidine-3-ol

https://huagongshe.com/reaction/1923330

Reaction equation

Participants

RoleNameHCIDCharge
ReactantTrifluoroacetic acidHCID 6422—
Reactant3-[2-(2-Ethylbenzoimidazol-1-yl)-9-methyl-6-morpholin-4-yl-9H-purin-8-yl]-3-hydroxy-azetidine-1-carboxylic acid tert-butyl esterHCID 59605874—
SolventDichloromethaneHCID 6344—
Product3-[2-(2-Ethylbenzoimidazol-1-yl)-9-methyl-6-morpholin-4-yl-9H-purin-8-yl]azetidine-3-olHCID 5960607489.3%

Reaction Steps

To a solution of 3-[2-(2-ethylbenzoimidazol-1-yl)-9-methyl-6-morpholin-4-yl-9H-purin-8-yl]-3-hydroxyazetidine-1-carboxylic acid tert-butyl ester (620 mg, 1.16 mmol) in DCM (5 mL) was added TFA (2 mL) and the resulting mixture allowed to stir for 1.5 h at r.t. The reaction mixture was loaded onto an Isolute® SCX-2 cartridge which was washed with DCM and MeOH and the product eluted with 2M NH3/MeOH affording 3-[2-(2-Ethylbenzoimidazol-1-yl)-9-methyl-6-morpholin-4-yl-9H-purin-8-yl]azetidine-3-ol as a yellow oil (450 mg, 89%). LCMS: (method A): RT 1.84 min [M+H]+ 435.2

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08173650B2
Source datasetuspto-grants-2012_05
ORD IDord-3fef9dffa6144484bb982eb669fdb693
Source noteuspto-grants-2012_05