1269662-79-4

Basic information

• Product Name: diethyl ({[4-({3-chloro-4-[(pyridin-2-yl)methoxy]phenyl}amino)-3-cyano-7-ethoxyquinolin-6-yl]carbamoyl}methyl)phosphonate
• Synonyms: diethyl ({[4-({3-chloro-4-[(pyridin-2-yl)methoxy]phenyl}amino)-3-cyano-7-ethoxyquinolin-6-yl]carbamoyl}methyl)phosphonate
• CAS NO: 1269662-79-4
• Molecular Weight: 624.033
• Mol File: 1269662-79-4.mol
• Article Data: 6

Chemical Properties

• CAS DataBase Reference: diethyl ({[4-({3-chloro-4-[(pyridin-2-yl)methoxy]phenyl}amino)-3-cyano-7-ethoxyquinolin-6-yl]carbamoyl}methyl)phosphonate(CAS DataBase Reference)
• NIST Chemistry Reference: diethyl ({[4-({3-chloro-4-[(pyridin-2-yl)methoxy]phenyl}amino)-3-cyano-7-ethoxyquinolin-6-yl]carbamoyl}methyl)phosphonate(1269662-79-4)
• EPA Substance Registry System: diethyl ({[4-({3-chloro-4-[(pyridin-2-yl)methoxy]phenyl}amino)-3-cyano-7-ethoxyquinolin-6-yl]carbamoyl}methyl)phosphonate(1269662-79-4)

Safety Data

• Hazardous Substances Data: 1269662-79-4(Hazardous Substances Data)

Upstream product

• 524955-09-7 3-chloro-4-(2-pyridylmethoxy)aniline 
• 848133-76-6 7-ethoxy-6-acetylamino-4-chloro-quinoline-3-carbonitrile 
• 867-13-0 diethoxyphosphoryl-acetic acid ethyl ester 
• 179687-79-7 2-((2-chloro-4-nitrophenoxy)methyl)pyridine 
• 6959-47-3 2-chloromethylpyridine hydrochloride 
• 619-08-9 2-chloro-4-nitrophenol 
• 915941-95-6 N-(4-[3-chloro-4-(pyridin-2-ylmethoxy)phenylamino]-3-cyano-7-ethoxyquinoline-6-yl)acetamide 
• 848139-78-6 6-amino-4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]-7-ethoxyquinoline-3-carbonitrile 
• 3095-95-2 diethylphosphonoacetic acid 

Downstream Products

• 698387-09-6 neratinib 
• 1397922-62-1 (E)-N-[4-[[3-chloro-4-(2-pyridylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolyl]-3-[(2R)-1-methylpyrrolidin-2-yl]prop-2-enamide L-malate 
• 1397922-61-0 (E)-N-[4-[[3-chloro-4-(2-pyridylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolyl]-3-[(2R)-1-methylpyrrolidin-2-yl]prop-2-enamide maleate 
• 1397922-61-0 (R,E)-N-(4-(3-chloro-4-(pyridine-2-ylmethoxy)phenylamino)-3-cyano-7-ethoxyquinoline-6-yl)-3-(1-methylpyrrolidinyl-2-yl)acrylamide dimaleate salt 
• 1269662-81-8 (E)-3-[(2S,4R)-4-(tert-butyl(dimethyl)silyl)oxy-1-methylpyrrolidin-2-yl]-N-[4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolyl]prop-2-enoylamine 
• 1269662-71-6 (E)-N-[4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolinyl]-3-[(2S,4R)-4-hydroxy-1-methyl-pyrrolidin-2-yl]propan-2-enoylamine 
• 1269662-74-9 (E)-N-[4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolinyl]-3-(1-methyl-2-piperidinyl)prop-2-enoylamine 
• 1269662-69-2 (E)-N-[4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolinyl]-3-[(2S)-1-methylpyrrolidin-2-yl]propan-2-enoylamine 
• 1269662-73-8 (E)-N-[4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolinyl]-3-[(2R)-1-methylpyrrolidin-2-yl]propan-2-enoylamine 
• 1269662-78-3 (E)-N-[4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolinyl]-3-(1-methylpyrrolidin-2-yl)-propan-2-enoylamine 
• 1269662-80-7 (2S)-2-[(E)-3-[[4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]-3-cyano-7-ethoxyquinolin-6-yl]amino]-3-oxopropen-1-yl]pyrrolidine-1-carboxylic acid tert-butyl ester 
• 1269662-70-5 (E)-N-[4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolinyl]-3-[(2S)-pyrrolidin-2-yl]propan-2-enoylamide 

Relevant articles and documents

The Wittig-Horner reaction for the synthesis of neratinib

The Wittig-Horner reaction is a classic method to get alkenes by reaction phosphonates with carbonyl compounds. In this study, it was used for the synthesis of the anticancer drug neratinib. In this method, ethyl diethoxyphosphinylacetate and dimethylaminoacetaldehyde diethylacetal, replacing (E)-4-(dimethylamino)but-2-enoyl acid hydrochloride and oxalyl chloride, were used to synthesize the 6-position side chain of neratinib.

4-quinazoline amine derivatives and their use

A 4-quinazoline amine derivative as represented by formula (1), a pharmaceutical composition comprising the derivative, and an application thereof in preparing medicine for curing cancer. The cancer is a drug-resistant cancer, preferably a cancer resisting an EGFR reversible inhibitor, and more preferably, a cancer resisting gefitinib, erlotinib or lapatinib; alternatively, the cancer carries EGFR mutation.

PHARMACEUTICALLY ACCEPTABLE SALT OF (E)-N-[4-[[3-CHLORO-4-(2-PYRIDYLMETHOXY)PHENYL]AMINO]-3-CYANO-7-ETHOXY-6-QUINOLYL]-3-[(2R)-1-METHYLPYRROLIDIN-2-YL]PROP-2-ENAMIDE, PREPARATION METHOD THEREOF, AND MEDICAL USE THEREOF

Provided as represented by formula (I) is a pharmaceutically acceptable salt of (E)-N-[4-[[3-chloro-4-(2-pyridylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolyl]-3-[(2R)-1-methylpyrrolidin-2-yl]prop-2-enamide, a preparation method thereof, and a use thereof as a therapeutic agent, and especially as a protein kinase inhibitor.