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ChemicalBook CAS DataBase List JAK3 INHIBITOR I
202475-60-3

JAK3 INHIBITOR I synthesis

5synthesis methods
-

Yield: 98%

Reaction Conditions:

in isopropyl alcohol at 85; for 2 h;

Steps:

16.1; 31.1 Step 1: 4-((6,7-dimethoxyquinazolin-4-yl)amino)phenol
A mixture of 4-chloro-6,7-dimethoxyquinazoline (1.00 g, 4.452 mmol, 1.00 equiv) and 4-aminophenol (583 mg, 5.342 mmol, 1.20 equiv) in isopropanol (15 mL) was stirred at 85°C for 2 h. After cooled to room temperature, the solid was collected by filtration, washed with methanol (15 mL x 2) and dried in vacuo to give 1.30 g (98%) of 4-(6,7-dimethoxyquinazolin-4- ylamino)phenol as an off-white solid. 1H-NMR (300 MHz, DMSO-rL, ppm): d 11.07 (s, 1H), 9.66 (s, 1H), 8.70 (s, 1H), 8.22 (s, 1H), 7.45-7.40 (m, 2H), 7.32 (s, 1H), 6.88-6.82 (m, 2H), 3.99 (s, 3H), 3.97 (s, 3H).

References:

RIBOSCIENCE LLC;HAWLEY, Ronald;KLUMPP, Klaus WO2020/140001, 2020, A1 Location in patent:Paragraph 0195; 0229

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