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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 535195Generated: October 31, 2026

4-Carboxy-1,2,3-triazole → HCID 178473661, compound

https://huagongshe.com/reaction/535195

Reaction equation

Participants

RoleNameHCIDCharge
Reactant4-Carboxy-1,2,3-triazoleHCID 140120—
ReactantMethanaminium, N-((dimethylamino)(3H-1,2,3-triazolo(4,5-b)pyridin-3-yloxy)methylene)-N-methyl-, hexafluorophosphate(1-) (1:1)HCID 9886157—
Reactant(2S,4R)-4-amino-5-biphenyl-4-yl-2-hydroxymethyl-2-methyl-pentanoic acid ethoxycarbonyloxymethyl esterHCID 68181053—
CatalystDiisopropylethylamineHCID 81531—
SolventDimethylformamideHCID 6228—
ProductHCID 178473661HCID 1784736618,161.3%

Reaction Steps

1,2,3-Triazole-4-carboxylic acid (14 mg, 124 nmol), DIPEA (86.3 mL, 496 nmol) and HATU (47.1 mg, 124 nmol) were combined in DMF (0.2 mL) and stirred for 5 minutes at room temperature. This was then combined with (2S,4R)-4-amino-5-biphenyl-4-yl-2-hydroxymethyl-2-methyl-pentanoic acid ethoxycarbonyloxymethyl ester (51 mg, 120 nmol). The resulting mixture was stirred for 15 minutes and the reaction was quenched with AcOH. The product purified by preparative HPLC and lyophilized to yield the title compound (5 mg; purity 90%). MS m/z [M+H]+ calc'd for C26H30N4O2, 511.21. found 511.6.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08853427B2
Source datasetuspto-grants-2014_10
ORD IDord-9e41ecabf94f4d708af3476f731d79a6
Source noteuspto-grants-2014_10