Gefitinib InterMediate B

A suspension of 4-((3-chloro-4-fluorophenyl)amino)-7- methoxyquinazolin-6-ol (20.00 g), KA suspension of 4-((3-chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-ol (20.00 g), KThe steps for the synthesis of intermediate compound 8: Refering to the formula IV, and according to the formula VI, compound 7 (478mg, 1.5mmol), 1-bromo-3-chloropropane (1.18g, 7.5mmol) and KN-dimethylformamidine, 0.72 g (6.15 mmol) of N '- [2-cyano-4, 5-bis (2-methoxyethoxy) phenyl] ) Of 3-aminophenylacetylene and 8 mL of acetic acid were reacted in a 50 mL reaction flask at 125 ° C for 1 hour and cooled to room temperature.20 mL of ice water was added to the mixture, the pH was adjusted to 10 with aqueous ammonia, and the mixture was stirred for 1 hour, suction filtered and the filter cake washed with water until neutral.The filter cake was dried to obtain 2.15 g of erlotinib in a yield of 91.5percent.General procedure: Followed the reference methods,

Molecular Weight:396.2
XLogP3:5
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:6
Rotatable Bond Count:7
Exact Mass:395.0603603
Monoisotopic Mass:395.0603603
Topological Polar Surface Area:56.3
Heavy Atom Count:26
Complexity:437
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes