Hydrochloric Acid → (R)-7-ethyl-8-isopropyl-2-[2-methoxy-4-(4-pyrrolidin-1-yl-piperidin-1-yl)-phenylamino]-5-methyl-7,8-dihydro-5H-pteridin-6-one

HRID 2222127Notes

Reaction equation

Cl[C:2]1[N:11]=[CH:10][C:9]2[N:8]([CH3:12])[C:7](=[O:13])[C@@H:6]([CH2:14][CH3:15])[N:5]([CH:16]([CH3:18])[CH3:17])[C:4]=2[N:3]=1.Cl.[CH3:20][O:21][C:22]1[CH:27]=[C:26]([N:28]2[CH2:33][CH2:32][CH:31]([N:34]3[CH2:38][CH2:37][CH2:36][CH2:35]3)[CH2:30][CH2:29]2)[CH:25]=[CH:24][C:23]=1[NH2:39]>C(O)C>[CH2:14]([C@H:6]1[N:5]([CH:16]([CH3:18])[CH3:17])[C:4]2[N:3]=[C:2]([NH:39][C:23]3[CH:24]=[CH:25][C:26]([N:28]4[CH2:33][CH2:32][CH:31]([N:34]5[CH2:38][CH2:37][CH2:36][CH2:35]5)[CH2:30][CH2:29]4)=[CH:27][C:22]=3[O:21][CH3:20])[N:11]=[CH:10][C:9]=2[N:8]([CH3:12])[C:7]1=[O:13])[CH3:15]

Participants

Conditions

Temperature: 100 °C

Procedure

50 mg (0.186 mmol) (R)-2-chloro-7-ethyl-8-isopropyl-5-methyl-7,8-dihydro-5H-pteridin-6-one are dissolved in 0.5 ml of ethanol and 1 ml distilled water, combined with 136 μl of a 33% aqueous hydrochloric acid and 56 mg (0.203 mmol) 2-methoxy-4-(4-pyrrolidin-1-yl-piperidin-1-yl)-phenylamine (method 1) and stirred for 3 h at 100° C.

Workup

distillation1 ml distilled water

Sources & evidence

ORD record: ord-0b2d8392d56243cea43e020ab8bdce4b
Source dataset: uspto-grants-2008_05
DOI: 10.6084/m9.figshare.5104873.v1
Patent number: US07371753B2

Reaction notes

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