Hydrochloric Acid → HCID 10032356, compound

HRID 2217136Notes

Reaction equation

HRID 2217136 reaction equation
[P:1]([O:13][CH2:14][C@@H:15]1[CH2:19][CH2:18][CH2:17][N:16]1[CH2:20][CH2:21][CH2:22][O:23][C:24]1[CH:33]=[C:32]2[C:27]([C:28]([NH:34][C:35]3[S:36][C:37]([CH2:40][C:41]([NH:43][C:44]4[CH:49]=[CH:48][C:47]([F:50])=[C:46]([F:51])[CH:45]=4)=[O:42])=[CH:38][N:39]=3)=[N:29][CH:30]=[N:31]2)=[CH:26][C:25]=1[O:52][CH3:53])([O:8]C(C)(C)C)([O:3]C(C)(C)C)=[O:2].Cl>O1CCOCC1>[P:1]([OH:3])([OH:8])([O:13][CH2:14][C@@H:15]1[CH2:19][CH2:18][CH2:17][N:16]1[CH2:20][CH2:21][CH2:22][O:23][C:24]1[CH:33]=[C:32]2[C:27]([C:28]([NH:34][C:35]3[S:36][C:37]([CH2:40][C:41]([NH:43][C:44]4[CH:49]=[CH:48][C:47]([F:50])=[C:46]([F:51])[CH:45]=4)=[O:42])=[CH:38][N:39]=3)=[N:29][CH:30]=[N:31]2)=[CH:26][C:25]=1[O:52][CH3:53])=[O:2]

Participants

4

Reactant 2

HCID 313Hydrochloric AcidHCID 86603909HCID 86603909, compound

Product 1

HCID 10032356HCID 10032356, compoundYield 90.1%

Reagents, catalysts & solvents 1

HCID 312751,4-DioxaneSolvent2×

Procedure

Di(tert-butyl) ((2S)-1-(3-((4-((5-(2-((3,4-difluorophenyl)amino)-2-oxoethyl)-1,3-thiazol-2-yl)amino)-6-methoxyquinazolin-7-yl)oxy)propyl)pyrrolidin-2-yl)methyl phosphate (537 mg, 0.69 mmol) in dioxane (10 ml) was treated with a solution of HCl (4N) in dioxane (1.2 ml) at ambient temperature for 15 hours. The solid was recovered by filtration, washed with dioxane, dried under vacuum at 50° C. to give the title compound (413 mg, 81% yield):

Workup

  1. filtrationThe solid was recovered by filtration
  2. washwashed with dioxane
  3. customdried under vacuum at 50° C.

Sources & evidence

ORD record
ord-05f78ae8dbab48d99dd4b710a13b22b3
Source dataset
uspto-grants-2008_08
Patent number
US07407946B2

Reaction notes

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