(5-Carbamoylthiophen-3-yl)boronic acid → 4-{8-[4-(4-(Cyclopropylmethyl)piperazin-1-yl)-phenylamino]-[1,2,4]triazolo[1,5-a]pyrazin-5-yl}thiophene-2-carboxylic acid amide

HRID 605932Notes

Reaction equation

HRID 605932 reaction equation
[CH:1]1([CH2:4][N:5]2[CH2:10][CH2:9][N:8]([C:11]3[CH:16]=[CH:15][C:14]([NH:17][C:18]4[C:19]5[N:20]([N:29]=[CH:30][N:31]=5)[C:21]([C:24]5[CH:25]=NNC=5)=[CH:22][N:23]=4)=[CH:13][CH:12]=3)[CH2:7][CH2:6]2)[CH2:3][CH2:2]1.[NH2:32][C:33]([C:35]1[S:36]C=C(B(O)O)[CH:39]=1)=[O:34]>>[CH:1]1([CH2:4][N:5]2[CH2:10][CH2:9][N:8]([C:11]3[CH:12]=[CH:13][C:14]([NH:17][C:18]4[C:19]5[N:20]([N:29]=[CH:30][N:31]=5)[C:21]([C:24]5[CH:39]=[C:35]([C:33]([NH2:32])=[O:34])[S:36][CH:25]=5)=[CH:22][N:23]=4)=[CH:15][CH:16]=3)[CH2:7][CH2:6]2)[CH2:2][CH2:3]1

Participants

3

Reactant 2

HCID 67047388(5-Carbamoylthiophen-3-yl)boronic acidHCID 135900377{4-[4-(Cyclopropylmethyl)piperazin-1-yl]phenyl}-[5-(1H-pyrazol-4-yl)-[1,2,4]triazolo[1,5-a]pyrazin-8-yl]amine

Product 1

HCID 248886114-{8-[4-(4-(Cyclopropylmethyl)piperazin-1-yl)-phenylamino]-[1,2,4]triazolo[1,5-a]pyrazin-5-yl}thiophene-2-carboxylic acid amide

Procedure

This compound may be prepared using methods as described for Compound 46, using 2-(aminocarbonyl)thiophene-4-boronic acid. LCMS: Rt=0.93 (95%), m/z (ESI) 475 (M+H)+.

Workup

  1. customThis compound may be prepared

Sources & evidence

ORD record
ord-819a7f3d0c234849bc03f419f6138704
Source dataset
uspto-grants-2011_03
Patent number
US07915256B2

Reaction notes

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