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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 735533Generated: October 29, 2026

Glyoxylic acid, monohydrate → 2-(1-(bis(tert-Butoxycarbonyl)amino)isoquinolin-6-ylamino)-2-(4-(4-(3-((tert-butoxycarbonyl(methyl)amino)methyl)-4-(ethylsulfonyl)phenylamino)-4-oxobutyl)phenyl)acetic acid

https://huagongshe.com/reaction/735533

Reaction equation

Participants

RoleNameHCIDCharge
ReactantGlyoxylic acid, monohydrateHCID 15620607—
Reactant4-(4-(3-((tert-Butoxycarbonyl(methyl)amino)methyl)-4-(ethylsulfonyl)phenylamino)-4-oxobutyl)phenylboronic acidHCID 57842904—
Reactanttert-butyl N-(6-aminoisoquinolin-1-yl)-N-[(tert-butoxy)carbonyl]carbamateHCID 58717298—
Product2-(1-(bis(tert-Butoxycarbonyl)amino)isoquinolin-6-ylamino)-2-(4-(4-(3-((tert-butoxycarbonyl(methyl)amino)methyl)-4-(ethylsulfonyl)phenylamino)-4-oxobutyl)phenyl)acetic acidHCID 57842708—

Reaction Steps

Using a procedure analogous to that used to prepare 2D, 17D (0.130 g, 0.25 mmol) was reacted with Intermediate 1 (0.090 g, 0.25 mmol) and glyoxylic acid monohydrate (0.027 g, 0.29 mmol) to give, after purification by reverse phase HPLC, 17E (109 mg, 49%). MS (ESI) m/z 890.1 (M+H)+.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS07592331B2
Source datasetuspto-grants-2009_09
ORD IDord-5a25074e37de4ecf93c3dbcb8a13c8d5
Source noteuspto-grants-2009_09