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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 2091872Generated: October 27, 2026

1-(tert-Butyldimethylsilyl)-5-fluoro-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indole → 4-(1-((2-(5-fluoro-1H-indol-4-yl)-4-morpholinopyrido[3,2-d]pyrimidin-6-yl)methyl)azetidin-3-yl)piperazin-2-one

https://huagongshe.com/reaction/2091872

Reaction equation

Participants

RoleNameHCIDCharge
Reactant1-(tert-Butyldimethylsilyl)-5-fluoro-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indoleHCID 57506725—
Reactant4-(1-((2-Chloro-4-morpholinopyrido[3,2-d]pyrimidin-6-yl)methyl)azetidin-3-yl)piperazin-2-oneHCID 58405021—
Product4-(1-((2-(5-fluoro-1H-indol-4-yl)-4-morpholinopyrido[3,2-d]pyrimidin-6-yl)methyl)azetidin-3-yl)piperazin-2-oneHCID 53378471—

Reaction Steps

4-(1-((2-chloro-4-morpholinopyrido[3,2-d]pyrimidin-6-yl)methyl)azetidin-3-yl)piperazin-2-one (87 mg) was reacted with 1-(tert-butyldimethylsilyl)-5-fluoro-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indole via General Procedure A to produce 46.1 mg of 127 following reverse phase HPLC purification. MS (Q1) 517.3 (M)+

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08440651B2
Source datasetuspto-grants-2013_05
ORD IDord-1ef1cb19937d40d4a1ac2662cab0d717
Source noteuspto-grants-2013_05