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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 510118Generated: October 26, 2026

Azetidine → 6-(Azetidin-1-yl)-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-7-methyl-7,9-dihydro-8H-purin-8-one

https://huagongshe.com/reaction/510118

Reaction equation

Participants

RoleNameHCIDCharge
ReactantAzetidineHCID 10422—
Reactant2-[1-(2-Fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-6-iodo-7-methyl-7,9-dihydro-8H-purin-8-oneHCID 86720052—
SolventN-methyl-2-pyrrolidoneHCID 13387—
Product6-(Azetidin-1-yl)-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-7-methyl-7,9-dihydro-8H-purin-8-oneHCID 569289485.2%

Reaction Conditions

Temperature150 °C

Reaction Steps

200 mg (0.399 mmol) of the compound obtained in example 107 were dissolved in N-methylpyrrolidone (3 ml) and admixed with 1.00 g (17.514 mmol) of azetidine, and then heated in a microwavable flask with septum in a microwave at 150° C. for 5 h. The mixture was purified by means of preparative HPLC (acetonitrile:water (+0.05% formic acid) gradient). 9 mg of the title compound were obtained (5% of theory).

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS09096592B2
Source datasetuspto-grants-2015_08
ORD IDord-2dd36de19b6b426391d8c5d1eaabbe84
Source noteuspto-grants-2015_08