Neratinib

$ 7.00 /1KG

Min. Order1KG
Purity99%
Cas No 698387-09-6
Supply Ability1000KG
Update time2019-07-06

career henan chemical co

7YR

China

Chemical Properties

Product Name	Neratinib
CAS No	698387-09-6
EC-No
Min. Order	1KG
Purity	99%
Supply Ability	1000KG
Release date	2019/07/06

JD607

Product Name:	Neratinib
Synonyms:	(2e)-n-[4-[[3-chloro-4-[(pyridin-2-yl)methoxy]phenyl]amino]-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide;neratinib;(E)-N-[4-[3-Chloro-4-[(2-pyridinyl)methoxy]anilino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide;N-(4-(3-Chloro-4-(2-pyridinylmethoxy)anilino)-3-cyano-7-ethoxy-6-quinolyl)-4-(dimethylamino)-2-butenamide;Unii-jjh94R3pwb;Neratinib(HKI-272);(2E)-N-[4-[[3-chloro-4-(2-pyridinylMethoxy)phenyl]aMino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(diMethylaMino)-2-butenaMide;(2e)-n-(4-((3-chloro-4-((pyridin-2-yl)Methoxy)phenyl)aMino)-3-cyano-7-ethoxyquinolin-6-yl)-4-(diMethylaMino)but-2-enaMide neratinib
CAS:	698387-09-6
MF:	C30H29ClN6O3
MW:	557.04266
EINECS:	1308068-626-2
Product Categories:	Antineoplastic;Anti-cancer & immunity;Inhibitors;API
Mol File:	698387-09-6.mol

Neratinib Chemical Properties

density

1.33

Safety Information

HS Code

29334900

MSDS Information

Neratinib Usage And Synthesis

New anticancer drug

Neratinib developed by US Wyeth company is an irreversible epidermal growth factor receptor(EGFR) inhibitor. It is a multiple target point of small molecule tyrosine kinase inhibitors to HER 2 and HER1 after Lapatinib, and is an irreversible ErbB receptor tyrosine kinase inhibitor. Neratinib could selectively inhibit HER-1 and HER-2 of EGFR family(IC50 was 92 nmol/L and 59 nmol/L, respectively). Clinical research showed that Neratinib exerted significant therapeutic effect on non-small cell lung cancer, colon cancer, and breast cancer.
The phaseⅡclinical trial indicated that Neratinib showed good efficacy and tolerance to HER-2 positive patients with advanced breast cancer who had been received or not Trastuzumab treatment.
The phase Ⅲ breast cancer clinical trial was complete in September 2014. The data indicated that the efficacy of Neratinib was better than Roche's Herceptin in treatment of HER-2 positive early breast cancer.
The above information is edited by the Chemicalbook of Liu Yujie.

Synthesis pathways

3-chloro-4-(pyridin-2-yl-methoxy)-aniline (2) and N-(4-chloro-3-cyano-7-ethoxy-quinolin-6-yl)-acetamide (3) are used as raw material to prepare N-[4-[3-chloro-4-(pyridin-2-yl-methoxy) anilino]-3-cyano-7-ethoxy-quinolin-6-yl] acetamide (4) by nucleophilic substitution. Deprotection of 4 was under the effect of hydrochloric acid, then was precipitated the free base in methanol solution of potassium carbonate to prepare 6-amino-3-cyano-4-[3-chloro-4-(pyridin-2-yl-methoxy) anilino]-7-ethoxy-quinoline (5). Neratinib(1) was obtained by condensation of 5 and acyl chloride which was prepared by trans-4-dimethylamino-crotonic acid hydrochloride (6).