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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 74554Generated: October 25, 2026

O-(Benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium tetrafluoroborate → 6-[4-(7-Methoxy-2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-5-methyl-pyrimidine-4-carboxylic acid

https://huagongshe.com/reaction/74554

Reaction equation

Participants

RoleNameHCIDCharge
ReactantO-(Benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium tetrafluoroborateHCID 2733207—
Reactant5-FluoroindolineHCID 2774463—
ReactantTert. butyl 6-[4-(7-methoxy-2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-5-methyl-pyrimidin-4-carboxylateHCID 58386534—
SolventDimethylformamideHCID 6228—
Product6-[4-(7-Methoxy-2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-5-methyl-pyrimidine-4-carboxylic acidHCID 58386435—

Reaction Steps

70 mg (0.17 mmol) tert. butyl 6-[4-(7-methoxy-2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-5-methyl-pyrimidin-4-carboxylate, 26 mg (0.19 mmol) 5-fluoroindoline, 61 mg (0.19 mmol) TBTU and 27 μL (0.19 mmol) TEA were stirred in 1.0 mL DMF for 3 h at RT. The reaction mixture was purified by HPLC. The product-containing fractions were combined and freeze-dried.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08829006B2
Source datasetuspto-grants-2014_09
ORD IDord-a503c57dd4264e0c8f32ab98bd540b0c
Source noteuspto-grants-2014_09