Diisopropylethylamine → 2-(3,5-Bis-(4-fluoro-phenyl)-(1,2,4)triazol-1-yl)-1-(4-(4-methoxy-pyridin-2-yl)-piperazin-1-yl)-ethanone

Participants

Role	Name	HCID	Charge
Reactant	Diisopropylethylamine	HCID 81531	—
Reactant	O-(Benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium tetrafluoroborate	HCID 2733207	—
Reactant	1-(4-Methoxypyridin-2-yl)piperazine	HCID 22648132	—
Reactant	(3,5-bis-(4-Fluoro-phenyl)-(1,2,4)triazol-1-yl)-acetic acid	HCID 86686517	—
Solvent	Dimethylformamide	HCID 6228	—
Product	2-(3,5-Bis-(4-fluoro-phenyl)-(1,2,4)triazol-1-yl)-1-(4-(4-methoxy-pyridin-2-yl)-piperazin-1-yl)-ethanone	HCID 71668166	60.3%

Reaction Steps

32 mg (3,5-bis-(4-fluoro-phenyl)-(1,2,4)triazol-1-yl)-acetic acid was dissolved in 2 mL DMF. 39 mg TBTU and 53 μL DIPEA were added to this solution and the mixture was stirred for a few minutes at RT. Then 24 mg 1-(4-methoxy-pyridin-2-yl)-piperazine was added. The mixture was stirred 1 h at RT. The reaction-solution was evaporated and the residue was purified by HPLC to give 30 mg of the desired compound. Rt: 1.68 (method C), (M+H)+: 491

Provenance & Evidence

DOI	10.6084/m9.figshare.5104873.v1
Patent number	US08889677B2
Source dataset	uspto-grants-2014_11
ORD ID	ord-5c3418c407564ac080c60a1abbb0c8f5
Source note	uspto-grants-2014_11