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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 736949Generated: October 29, 2026

2-Methyl-5-piperidin-4-yl-2,5-diaza-bicyclo[2.2.1]heptane → (S)-2-(4-amino-3-chloro-5-trifluoromethyl-benzyl)-1-[4-(5-methyl-2,5-diaza-bicyclo[2.2.1]hept-2-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dione

https://huagongshe.com/reaction/736949

Reaction equation

Participants

RoleNameHCIDCharge
Reactant2-Methyl-5-piperidin-4-yl-2,5-diaza-bicyclo[2.2.1]heptaneHCID 59814499—
Reactant(S)-2-(4-amino-3-chloro-5-trifluoromethyl-benzyl)-4-oxo-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butanoic acidHCID 68591515—
SolventTriethylamineHCID 8471—
Product(S)-2-(4-amino-3-chloro-5-trifluoromethyl-benzyl)-1-[4-(5-methyl-2,5-diaza-bicyclo[2.2.1]hept-2-yl)-piperidin-1-yl]-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butan-1,4-dioneHCID 57848361—

Reaction Steps

Prepared analogously to Example 10.26 from 100 mg (0.18 mmol) (S)-2-(4-amino-3-chloro-5-trifluoromethyl-benzyl)-4-oxo-4-[4-(2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-butanoic acid and 39.1 mg (0.2 mmol) 2-methyl-5-piperidin-4-yl-2,5-diaza-bicyclo[2.2.1]heptane using triethylamine as the base.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS07595312B2
Source datasetuspto-grants-2009_09
ORD IDord-0df9ce69f7e748f1a878a9faac08e67c
Source noteuspto-grants-2009_09