Back
HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1051004Generated: October 31, 2026

Methylamine → tert-butyl ((5-(2-fluorophenyl)-1-((3-(2-(methylamino)-2-oxoethoxy)phenyl)sulfonyl)-1H-pyrrol-3-yl)methyl)(methyl)carbamate

https://huagongshe.com/reaction/1051004

Reaction equation

Participants

RoleNameHCIDCharge
ReactantMethylamineHCID 6329—
Reactantmethyl 2-(3-((4-(((tert-butoxycarbonyl)(methyl)amino)methyl)-2-(2-fluorophenyl)-1H-pyrrol-1-yl)sulfonyl)phenoxy)acetateHCID 90168695—
SolventMethanolHCID 887—
Producttert-butyl ((5-(2-fluorophenyl)-1-((3-(2-(methylamino)-2-oxoethoxy)phenyl)sulfonyl)-1H-pyrrol-3-yl)methyl)(methyl)carbamateHCID 90168692—

Reaction Conditions

Temperature40 °C

Reaction Steps

Methyl 2-(3-((4-(((tert-butoxycarbonyl)(methyl)amino)methyl)-2-(2-fluorophenyl)-1H-pyrrol-1-yl)sulfonyl)phenoxy)acetate 1i (110 mg, 0.20 mmol) was dissolved in 10 mL of a solution of methylamine in methanol (33%), and the reaction solution was heated up to 40° C. and stirred for 2 h. The reaction solution was concentrated under reduced pressure to obtain the title product tert-butyl ((5-(2-fluorophenyl)-1-((3-(2-(methylamino)-2-oxoethoxy)phenyl)sulfonyl)-1H-pyrrol-3-yl)methyl)(methyl)carbamate 1j (60 mg, a yellow oil), which was used directly in the next step.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS09388133B2
Source datasetuspto-grants-2016_07
ORD IDord-33a5d5c86c9c479d9f3113ab7915e39f
Source noteuspto-grants-2016_07