Trifluoroacetic acid → 7-Azetidin-1-yl-4-[3-(5-hydroxymethyl-[1,2,3]triazol-1-yl)-phenyl]-8-trifluoromethyl-1,3-dihydro-benzo[b][1,4]diazepin-2-one

HRID 1265806Notes

Reaction equation

HRID 1265806 reaction equation
C(OC(=O)[NH:7][C:8]1[CH:13]=[C:12]([N:14]2[CH2:17][CH2:16][CH2:15]2)[C:11]([C:18]([F:21])([F:20])[F:19])=[CH:10][C:9]=1[NH:22][C:23](=[O:46])[CH2:24][C:25](=O)[C:26]1[CH:31]=[CH:30][CH:29]=[C:28]([N:32]2[C:36]([CH2:37][O:38]C3CCCCO3)=[CH:35][N:34]=[N:33]2)[CH:27]=1)(C)(C)C.C(O)(C(F)(F)F)=O>C(Cl)Cl>[N:14]1([C:12]2[C:11]([C:18]([F:20])([F:21])[F:19])=[CH:10][C:9]3[NH:22][C:23](=[O:46])[CH2:24][C:25]([C:26]4[CH:31]=[CH:30][CH:29]=[C:28]([N:32]5[C:36]([CH2:37][OH:38])=[CH:35][N:34]=[N:33]5)[CH:27]=4)=[N:7][C:8]=3[CH:13]=2)[CH2:15][CH2:16][CH2:17]1

Participants

4

Reactant 2

HCID 6422Trifluoroacetic acidHCID 86586846HCID 86586846, compound

Product 1

HCID 186135177-Azetidin-1-yl-4-[3-(5-hydroxymethyl-[1,2,3]triazol-1-yl)-phenyl]-8-trifluoromethyl-1,3-dihydro-benzo[b][1,4]diazepin-2-one

Reagents, catalysts & solvents 1

HCID 6344DichloromethaneSolvent

Procedure

The title compound was prepared from (RS)-[5-azetidin-1-yl-2-(3-oxo-3-{3-[5-(tetrahydro-pyran-2-yloxymethyl)-[1,2,3]triazol-1-yl]-phenyl}-propionylamino)-4-trifluoromethyl-phenyl]-carbamic acid tert.-butyl ester (Example M54) by treatment with TFA in CH2Cl2 according to the general procedure N. Obtained as a yellow solid (182 mg).

Sources & evidence

ORD record
ord-7a65ffa6e1aa443eb54ea847af13b787
Source dataset
uspto-grants-2003_04
Patent number
US06544985B2

Reaction notes

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