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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 2170391Generated: October 30, 2026

(3bS,4aR)-5,5-Difluoro-3b,4,4a,5-tetrahydro-3-(trifluoromethyl)-1H-cyclopropa(3,4)cyclopenta(1,2-c)pyrazole-1-acetic acid → N-((S)-1-(5-amino-6-chloro-3-(4-chloro-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/2170391

Reaction equation

Participants

RoleNameHCIDCharge
Reactant(3bS,4aR)-5,5-Difluoro-3b,4,4a,5-tetrahydro-3-(trifluoromethyl)-1H-cyclopropa(3,4)cyclopenta(1,2-c)pyrazole-1-acetic acidHCID 90281286—
Reactant2-((3bS,4aR)-3-(difluoromethyl)-5,5-difluoro-3b,4,4a,5-tetrahydro-1H-cyclopropa[3,4]cyclopenta[1,2-c]pyrazol-1-yl)acetic acidHCID 90281289—
Reactant(S)-tert-butyl (1-(5-amino-6-chloro-3-(4-chloro-1-methyl-3-(methylsulfonamido)-1H-indazol-7-yl)pyridin-2-yl)-2-(3,5-difluorophenyl)ethyl)carbamateHCID 90290154—
ProductN-((S)-1-(5-amino-6-chloro-3-(4-chloro-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 90281233—

Reaction Steps

Compound 54 was prepared from compound 53A according to the method presented for the synthesis of Example 49 substituting 2-((3bS,4aR)-5,5-difluoro-3-(trifluoromethyl)-3b,4,4a,5-tetrahydro-1H-cyclopropa[3,4]cyclopenta[1,2-c]pyrazol-1-yl)acetic acid for 2-((3bS,4aR)-3-(difluoromethyl)-5,5-difluoro-3b,4,4a,5-tetrahydro-1H-cyclopropa[3,4]cyclopenta[1,2-c]pyrazol-1-yl)acetic acid to provide 13 mg of title compound: 1H NMR (400 MHz, Methanol-d4) δ 7.12-6.94 (m, 2H), 6.81-6.60 (m, 1H), 6.55-6.35 (m, 2H), 6.25 (d, 1H), 5.01-4.90 (m, 1H), 4.76 (t, 2H), 3.41 (s, 2H), 3.24 (d, 3H), 3.15-2.88 (m, 3H), 2.48 (q, 2H), 1.47-1.38 (m, 1H), 1.16-1.04 (m, 1H). MS (m/z) 805 [M+H]+.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS09050344B2
Source datasetuspto-grants-2015_06
ORD IDord-eaac06b06e554c56b93346ce61a7df9b
Source noteuspto-grants-2015_06