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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1027429Generated: October 29, 2026

Azetidine → 2-[4-(4-Azetidin-1-yl-cyclohexyl)-2-fluoro-phenyl]-1-oxo-2,8-diaza-spiro[4.5]decane-8-carboxylic acid tert-butyl ester

https://huagongshe.com/reaction/1027429

Reaction equation

Participants

RoleNameHCIDCharge
ReactantAzetidineHCID 10422—
Reactant2-[2-Fluoro-4-(4-methanesulfonyloxy-cyclohexyl)-phenyl]-1-oxo-2,8-diaza-spiro[4.5]decane-8-carboxylic acid tert-butyl esterHCID 86678096—
Product2-[4-(4-Azetidin-1-yl-cyclohexyl)-2-fluoro-phenyl]-1-oxo-2,8-diaza-spiro[4.5]decane-8-carboxylic acid tert-butyl esterHCID 54591844—

Reaction Steps

The title compound was synthesized in the same manner as Example 13 by condensing 2-[2-fluoro-4-(4-methanesulfonyloxy-cyclohexyl)-phenyl]-1-oxo-2,8-diaza-spiro[4.5]decane-8-carboxylic acid tert-butyl ester (Intermediate 28) (150 mg, 0.3 mmol, 1 equiv.) with azetidine (67.8 mg, 1.19 mmol) to obtain 55 mg (85% yield) of the compound.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08735385B2
Source datasetuspto-grants-2014_05
ORD IDord-264821d244164b969cf34c06207a99e6
Source noteuspto-grants-2014_05