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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 1481933Generated: October 30, 2026

Terephthaloyl chloride → (2S)-N-[(3S)-5-[[1-(2-Cyanophenyl)indazol-3-yl]methyl]-1-[4-[(3S)-5-[[1-(2-cyanophenyl)indazol-3-yl]methyl]-3-[[(2S)-2-(methylamino)propanoyl]amino]-4-oxo-2,3-dihydro-1,5-benzodiazepine-1-carbonyl]benzoyl]-4-oxo-2,3-dihydro-1,5-benzodiazepin-3-yl]-2-(methylamino)propanamide dihydrochloride

https://huagongshe.com/reaction/1481933

Reaction equation

Participants

RoleNameHCIDCharge
ReactantTerephthaloyl chlorideHCID 7488—
Reactant((S)-1-{(S)-1-[1-(2-Cyano-phenyl)-1H-indazol-3-ylmethyl]-2-oxo-2,3,4,5-tetrahydro-1H-benzo[b][1,4]diazepin-3-ylcarbamoyl}-ethyl)-methyl-carbamic acid tert-butyl esterHCID 90220958—
Product(2S)-N-[(3S)-5-[[1-(2-Cyanophenyl)indazol-3-yl]methyl]-1-[4-[(3S)-5-[[1-(2-cyanophenyl)indazol-3-yl]methyl]-3-[[(2S)-2-(methylamino)propanoyl]amino]-4-oxo-2,3-dihydro-1,5-benzodiazepine-1-carbonyl]benzoyl]-4-oxo-2,3-dihydro-1,5-benzodiazepin-3-yl]-2-(methylamino)propanamide dihydrochlorideHCID 902210149.8%

Reaction Steps

In a similar manner to that described for Example 22, ((S)-1-{(S)-1-[1-(2-cyano-phenyl)-1H-indazol-3-ylmethyl]-2-oxo-2,3,4,5-tetrahydro-1H-benzo[b][1,4]diazepin-3-ylcarbamoyl}-ethyl)-methyl-carbamic acid tert-butyl ester (Intermediate 14) (262.9 mg, 0.443 mmol) and terephthaloyl chloride (45 mg, 0.222 mmol) were converted to the title compound (13 mg) as a white solid. LC-MS: 1118 (M+H).

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS09409888B2
Source datasetuspto-grants-2016_08
ORD IDord-92a9e4ea0e2240d6be73e34ae103be6c
Source noteuspto-grants-2016_08