Hanmi Pharm. Co., Ltd.

Hanmi Science Co., Ltd.

Daewoong Pharmaceutical Co., Ltd.

Keuk Chan Bang

Maeng Sup Kim

Young Gil Ahn

Bum Woo Park

Gwan Sun Lee

Jae Chul Lee

Young Ho Moon

Jong Won Choi

Yong Hoon An

Jong Woo Kim

Young Hoon Kim

Joon Seok Park

Young Jin Ham

Young Kil Chang

Han Kyong Kim

Mi Young Cha

Deok Ki Eom

Jae Hyuk Jung

Youn Jung Yoon

Se Young Kim

Yeon Im Lee

Young-Gil Ahn

Kyungik Lee

Wol Young Kim

Kyuhang Lee

Myoung-Sil Ko

Jaehyun Jung

The present invention relates to a novel method for preparing 1-(4-(4-(3,4-dichloro-2-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)piperidin-1-yl)prop-2-en-1-one in a simpler process as compared with conventional methods by allowing 4-(3,4-dichloro-2-fluorophenylamino)-7-methoxyquinazolin-6-ol to react with an N-acyl piperidine derivative in an inert polar protic solvent in the presence of a base.

Method for preparing 1-(4-(4-(3,4-dichloro-2-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)piperidin-1-yi)prop-2-en-1-one

A method for preparing tetrazole methanesulfonic acid salts includes an acylation reaction using a novel 4-iodine-4H-chromene-2-carbothionic acid S-benzothiazole-2-yl ester. The method is advantageous that it can shorten a reaction time and improve safety as compared to conventional methods, and can prepare high-purity tetrazole methanesulfonic acid salts at a high yield rate without using a column chromatography method.

Method for preparing tetrazole methanesulfonic acid salts, and novel compound used in same

The present invention relates to an improved method for preparing 1-(4-(4-(3,4-dichloro-2-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)piperidin-1-yl)-prop-2-en-1-one hydrochloride, which selectively and effectively inhibits the growth of cancer cells induced by over-expression of an epidermal growth factor receptor (EGFR) and prevents the development of drug resistance caused by mutation of a tyrosine kinase, and intermediates used therein.

Method for preparing 1-(4-(4-(3,4-dichloro-2-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)piperidin-1-yl)-prop-2-en-1-one hydrochloride and intermediates used therein

The present invention relates to a novel quinazoline derivative compound having the formula (1) as follows: with the constituents defined in claim, and a pharmaceutically acceptable salt thereof as a multiplex inhibitor, a method for the preparation thereof, and a pharmaceutical composition and a therapeutic composition comprising same as an active ingredient. The inventive quinazoline derivative as a multiplex inhibitor can selectively and effectively inhibit diseases caused by the overactivity of a tyrosine kinase.

Quinazoline derivatives as a multiplex inhibitor and method for the preparation thereof

According to the present invention, a method for preparing tetrazole methanesulfonic acid salts comprises an acylation reaction using a novel 4-iodine-4H-chromene-2-carbothionic acid S-benzothiazole-2-yl ester. The method of the present invention can shorten a reaction time and improve safety as compared to conventional methods, and can prepare high-purity tetrazole methanesulfonic acid salts at a high yield rate without using a column chromatography method.

The bioavailability of an anticancer agent is enhanced when the anticancer agent is administered together with a pharmaceutical composition comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof.

P-glycoprotein inhibitor, method for preparing the same and pharmaceutical composition comprising the same

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Incheon, South Korea

Keuk Chan Bang