HCID 54759819, compound → Maleic Acid

HRID 473296Notes

Reaction equation

HRID 473296 reaction equation
[C:1]([OH:8])(=[O:7])/[CH:2]=[CH:3]\[C:4]([OH:6])=[O:5].[NH2:9][C:10]1[C:15]2[C:16]([C:19]3[CH:24]=[CH:23][C:22]([NH:25][C:26]([NH:28][C:29]4[CH:34]=[CH:33][CH:32]=[C:31]([F:35])[CH:30]=4)=[O:27])=[CH:21][CH:20]=3)=[CH:17][S:18][C:14]=2[C:13]([C:36]2[CH:37]=[N:38][N:39]([CH2:41][CH2:42][OH:43])[CH:40]=2)=[CH:12][N:11]=1>CN(C)C=O>[NH2:9][C:10]1[C:15]2[C:16]([C:19]3[CH:20]=[CH:21][C:22]([NH:25][C:26]([NH:28][C:29]4[CH:34]=[CH:33][CH:32]=[C:31]([F:35])[CH:30]=4)=[O:27])=[CH:23][CH:24]=3)=[CH:17][S:18][C:14]=2[C:13]([C:36]2[CH:37]=[N:38][N:39]([CH2:41][CH2:42][OH:43])[CH:40]=2)=[CH:12][N:11]=1.[C:1]([OH:8])(=[O:7])/[CH:2]=[CH:3]\[C:4]([OH:6])=[O:5]

Participants

4

Reactant 1

HCID 54759819HCID 54759819, compound

Product 2

HCID 444266Maleic AcidHCID 46207586Ilorasertib

Reagents, catalysts & solvents 1

HCID 6228DimethylformamideSolvent

Procedure

There is further provided a process for preparing N-(4-{4-amino-7-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]thieno[3,2-c]pyridin-3-yl}phenyl)-N′-(3-fluorophenyl)urea maleate in a solid crystalline form, wherein the crystalline form is Form VIII, comprising: a) providing a mixture comprising (i) N-(4-{4-amino-7-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]thieno[3,2-c]pyridin-3-yl}phenyl)-N′-(3-fluorophenyl)urea free base solid, dimethyl formamide, and maleic acid; b) causing N-(4-{4-amino-7-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]thieno[3,2-c]pyridin-3-yl}phenyl)-N′-(3-fluorophenyl)urea maleate crystalline Form VIII to exist in the mixture.

Workup

  1. customThere is further provided a process

Sources & evidence

ORD record
ord-7fcb0c7d6deb4b6195e87f607a168fff
Source dataset
uspto-grants-2014_01
Patent number
US08633317B2

Reaction notes

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