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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 2170381Generated: October 29, 2026

N-((S)-1-(6-chloro-3-(1-methyl-3-(methylsulfonamido)-1H-indazol-7-yl)pyridin-2-yl)-2-(3,5-difluorophenyl)ethyl)-2-((3bS,4aR)-5,5-difluoro-3-(trifluoromethyl)-3b,4,4a,5-tetrahydro-1H-cyclopropa[3,4]cyclopenta[1,2-c]pyrazol-1-yl)acetamide → N-((1S)-1-(6-(4-amino-2-oxopyrrolidin-1-yl)-3-(1-methyl-3-(methylsulfonamido)-1H-indazol-7-yl)pyridin-2-yl)-2-(3,5-difluorophenyl)ethyl)-2-((3bS,4aR)-5,5-difluoro-3-(trifluoromethyl)-3b,4,4a,5-tetrahydro-1H-cyclopropa[3,4]cyclopenta[1,2-c]pyrazol-1-yl)acetamide

https://huagongshe.com/reaction/2170381

Reaction equation

Participants

RoleNameHCIDCharge
ReactantN-((S)-1-(6-chloro-3-(1-methyl-3-(methylsulfonamido)-1H-indazol-7-yl)pyridin-2-yl)-2-(3,5-difluorophenyl)ethyl)-2-((3bS,4aR)-5,5-difluoro-3-(trifluoromethyl)-3b,4,4a,5-tetrahydro-1H-cyclopropa[3,4]cyclopenta[1,2-c]pyrazol-1-yl)acetamideHCID 90281204—
Reactanttert-Butyl (S)-(1-(3,6-dibromopyridin-2-yl)-2-(3,5-difluorophenyl)ethyl)carbamateHCID 90290190—
Reactant(S)-tert-butyl (1-(3-bromo-6-(3-hydroxy-3-methylazetidin-1-yl)pyridin-2-yl)-2-(3,5-difluorophenyl)ethyl)carbamateHCID 90290192—
ProductN-((1S)-1-(6-(4-amino-2-oxopyrrolidin-1-yl)-3-(1-methyl-3-(methylsulfonamido)-1H-indazol-7-yl)pyridin-2-yl)-2-(3,5-difluorophenyl)ethyl)-2-((3bS,4aR)-5,5-difluoro-3-(trifluoromethyl)-3b,4,4a,5-tetrahydro-1H-cyclopropa[3,4]cyclopenta[1,2-c]pyrazol-1-yl)acetamideHCID 90290137—

Reaction Steps

Compound 43B was prepared according to the method presented in the synthesis of compound 42G of Example 42 substituting N—((S)-1-(6-chloro-3-(1-methyl-3-(methylsulfonamido)-1H-indazol-7-yl)pyridin-2-yl)-2-(3,5-difluorophenyl)ethyl)-2-((3bS,4aR)-5,5-difluoro-3-(trifluoromethyl)-3b,4,4a,5-tetrahydro-1H-cyclopropa[3,4]cyclopenta[1,2-c]pyrazol-1-yl)acetamide (43A) for (S)-Atert-butyl (1-(3,6-dibromopyridin-2-yl)-2-(3,5-difluorophenyl)ethyl)carbamate (42F). 1H NMR (400 MHz, methanol-d4) δ 8.69-8.34 (m, 2H), 7.91-7.67 (m, 2H), 7.38-6.89 (m, 1H), 6.93-6.52 (m, 1H), 6.48-6.14 (m, 2H), 5.39-4.92 (m, 1H), 4.84-4.70 (m, 2H), 4.69-4.33 (m, 2H), 4.27 (m, 1H), 3.48-2.72 (m, 10H), 2.62-2.28 (m, 2H), 1.61-1.27 (m, 1H), 1.08 (m, 1H). MS (m/z) 820.00[M+H]+.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS09050344B2
Source datasetuspto-grants-2015_06
ORD IDord-af1cc4d16e22485c9efeecf915439732
Source noteuspto-grants-2015_06