A series of mono- and di-substituted quinazoline and pyrimidine derivatives based on the skeleton of erlotinib (an EGFR inhibitor) were synthesized and their bioactivities against hepatocellular carcinoma and human lung adenocarcinoma were evaluated.

Provided is a process for preparation of Crystalline Erlotinib HCl Form-SE characterized by X-ray powder diffraction pattern comprising at least 5 characteristic 2theta DEG peaks selected from the XRPD peak set of 5.60, 10.00, 11.40, 13.00, 13.50, 15.20, 18.40, 20.65, 21.86, 23.5, 31.80, 32.13, 32.80, 34.40 +- 0.20 2theta DEG , DSC isotherm comprising the endothermic peaks ranging between 213 to 217 DEG C (Peak -1) and 225 to 235 DEG C (Peak -2) and IR absorption characteristic peaks at approx...

The present invention provides a novel and stable hydrated form of erlotinib free base and a process for its preparation thereof. The present invention also provides a process for preparation of erlotinib hydrochloride crystalline polymorph a substantially free of polymorph B. The present invention further relates to erlotinib hydrochloride crystalline particles having mean particle size (D50) ranging from about 4 mum to 15 mum and 90 volume-% of the particles (D90) ranging from about 14 mum to ...

A novel crystal of antitumor drug erlotinib base and its preparation method are provided in the present invention. A preparation method of erlotinib hydrochloride with high-purity is also provided in the present invention.

Disclosed in the present invention are an Erlotinib hydrochloride polymorph and the preparation method therefor. In particular, disclosed in the present invention are an Erlotinib hydrochloride semihydrate polymorph with a purity >=95% and the preparation method therefor. The preparation method of the present invention is simple to operate and suitable for industrial production. The polymorph prepared by the preparation method of the invention has the advantages of good stability and high water ...

A process for the preparation of a salt of N-(3-ethynylphenyl)-67-bis(2-methoxyethoxy)quinazolin-4-amine comprising reacting a 4-halo-67-bis(2-methoxyethoxy) quinazoline with 3-aminophenyl acetylene or an acid salt thereof under acidic conditions to form the corresponding acid salt of N-(3-ethynylphenyl)-67-bis(2-methoxyethoxy)quinazolin-4-amine the process optionally further comprising converting the acid salt of N-(3-ethynylphenyl)-67-bis(2-methoxyethoxy)quinazolin-4-amine to N-(3-ethynylpheny...