ChemicalBook CAS DataBase List Erlotinib

Erlotinib synthesis

13synthesis methods

Product Name:Erlotinib
CAS Number:938185-06-9
Molecular formula:C16H11N3O2
Molecular Weight:277.28

6,7-Quinazolinediol, 4-[(3-ethynylphenyl)amino]-, 6,7-diacetate

938185-10-5
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938185-06-9
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Yield:938185-06-9 100%

Reaction Conditions:

with ammonium hydroxide in methanol at 20;

Steps:

9.5 Synthesis of 6,7-dihydroxy-4-anilinoquinazoline

3 g of the resulting product 6,7-diacetoxyl-4-anili- noquinazoline obtained in step 4 was dissolved in 40 ml of methanol, and then the mixture was added with 5 ml of aqua ammonia. The system was reacted at room temperature, and followed by TLC until the reaction finished. The reaction solution was concentrated in vacuum to obtain 2.3 g of the resulting product 6,7-dihydroxy-4-anilinoquinazoline(100%).10099] ‘H NMR (400 MHz, DMSO) ? 9.87 (bt, 1H), 8.52 (s, 1H), 8.00 (s, 1H), 7.85 (s, 1H), 7.41-7.19 (m, 4H), 4.27 (s, 1 H)10100] ESI mlz 278.0 (M+H)

References:

US2016/175453,2016,A1 Location in patent:Paragraph 0097; 0098; 0099; 00100