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Cas Database

698387-09-6

698387-09-6

Identification

  • Product Name:Neratinib

  • CAS Number: 698387-09-6

  • EINECS:811-237-1

  • Molecular Weight:557.052

  • Molecular Formula: C30H29ClN6O3

  • HS Code:29334900

  • Mol File:698387-09-6.mol

Synonyms:(E)-N-[4-[3-Chloro-4-[(2-pyridinyl)methoxy]anilino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide;(E)-N-[4-[[3-Chloro-4-((pyridin-2-yl)methoxy)phenyl]amino]-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)-2-butenamide;HKI 272;HKI-272(Neratinib);

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  • Manufacture/Brand:TRC
  • Product Description:Neratinib
  • Packaging:25mg
  • Price:$ 280
  • Delivery:In stock
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  • Manufacture/Brand:TRC
  • Product Description:Neratinib
  • Packaging:100mg
  • Price:$ 890
  • Delivery:In stock
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  • Manufacture/Brand:Matrix Scientific
  • Product Description:(E)-N-(4-(3-Chloro-4-(pyridin-2-yLmethoxy)phenylamino)-3-cyano-7-ethoxyquinolin-6-yl)-4-(dimethylamino)but-2-enamide 95%
  • Packaging:5g
  • Price:$ 5273
  • Delivery:In stock
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  • Manufacture/Brand:Matrix Scientific
  • Product Description:(E)-N-(4-(3-Chloro-4-(pyridin-2-yLmethoxy)phenylamino)-3-cyano-7-ethoxyquinolin-6-yl)-4-(dimethylamino)but-2-enamide 95%
  • Packaging:1g
  • Price:$ 1758
  • Delivery:In stock
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  • Manufacture/Brand:DC Chemicals
  • Product Description:Neratinib(HKI-272) >99%
  • Packaging:100 mg
  • Price:$ 200
  • Delivery:In stock
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  • Manufacture/Brand:DC Chemicals
  • Product Description:Neratinib(HKI-272) >99%
  • Packaging:1 g
  • Price:$ 800
  • Delivery:In stock
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  • Manufacture/Brand:DC Chemicals
  • Product Description:Neratinib(HKI-272) >99%
  • Packaging:250 mg
  • Price:$ 400
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  • Manufacture/Brand:Crysdot
  • Product Description:Neratinib 98+%
  • Packaging:250mg
  • Price:$ 275
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  • Manufacture/Brand:Chemtos
  • Product Description:Neratinibd5
  • Packaging:25 mg
  • Price:$ 1990
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  • Manufacture/Brand:ChemScene
  • Product Description:Neratinib 99.04%
  • Packaging:250mg
  • Price:$ 160
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Relevant articles and documentsAll total 15 Articles be found

Neratinib intermediate crystal as well as preparation method and application thereof

-

Paragraph 0088-0099, (2021/04/21)

The invention relates to a neratinib intermediate crystal as well as a preparation method and application thereof. The invention especially relates to a crystal form II of an intermediate A compound 6-amino-4-(3-chloro-4-(pyridine-2-substituted methoxy) aniline)-7-ethoxyquinoline carbonitrile. The crystal form II comprises diffraction peaks with diffraction angles 2 theta of 6.3 degrees, 7.8 degrees, 14.0 degrees, 15.1 degrees, 17.1 degrees, 18.8 degrees, 21.5 degrees, 22.2 degrees, 23.4 degrees and 27.5 degrees in an XRPD spectrum. When the intermediate crystal form II is used for preparing the neratinib, the dosage of a solvent can be remarkably reduced, the reaction time is shortened, the yield is increased, and meanwhile, the residual quantity of the intermediate A in a final product is remarkably reduced.

SOLID STATE FORMS OF NERATINIB AND SALTS THEREOF

-

Paragraph 0076, (2018/02/28)

Solid state forms of Neratinib and salts thereof, processes for preparation thereof and pharmaceutical compositions thereof are disclosed.

A to that of the preparation method of the Buddhist

-

Paragraph 0033-0057, (2017/10/06)

The invention relates to the field of pharmaceuticals, in particular to a preparation method of neratinib. The preparation method specifically includes: successively condensing 6-[(E)-4-(dimethylamino)-2-butenamido]-7-ethoxy-4-chloro-3-cyanoquinoline (I) with 2-chloro-4-aminophenol (II) and 2-(chloromethyl)pyridine hydrochloride (III) through an intermediate (E)-N-{4-[3-chloro-4-hydroxyanilino]3-cyano-7-ethoxy-6-quinoline}-4-dimethylamino-2-butenamide (IV). The materials in the preparation method are easy to obtain, and the preparation method is simple, green and economical and has greatly worthy of application.

Process route upstream and downstream products

Process route

6-amino-4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]-7-ethoxyquinoline-3-carbonitrile
848139-78-6

6-amino-4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]-7-ethoxyquinoline-3-carbonitrile

neratinib
698387-09-6

neratinib

Conditions
Conditions Yield
(E)-4-(dimethylamino)-2-butenoic acid hydrochloride; With oxalyl dichloride; N,N-dimethyl-formamide; In tetrahydrofuran; at 0 - 30 ℃; for 2h;
6-amino-4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]-7-ethoxyquinoline-3-carbonitrile; In tetrahydrofuran; 1-methyl-pyrrolidin-2-one; at 0 - 5 ℃; for 3 - 16h;
80%
6-amino-4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]-7-ethoxyquinoline-3-carbonitrile
848139-78-6

6-amino-4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]-7-ethoxyquinoline-3-carbonitrile

(E)-4-(dimethylamino)-2-butenoic acid hydrochloride
1130155-48-4

(E)-4-(dimethylamino)-2-butenoic acid hydrochloride

neratinib
698387-09-6

neratinib

Conditions
Conditions Yield
(E)-4-(dimethylamino)-2-butenoic acid hydrochloride; With oxalyl dichloride; N,N-dimethyl-formamide; In tetrahydrofuran; at 0 - 30 ℃; for 2.25h;
6-amino-4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]-7-ethoxyquinoline-3-carbonitrile; In tetrahydrofuran; 1-methyl-pyrrolidin-2-one; at 0 - 10 ℃; for 20.5h;
52%
diethyl ({[4-({3-chloro-4-[(pyridin-2-yl)methoxy]phenyl}amino)-3-cyano-7-ethoxyquinolin-6-yl]carbamoyl}methyl)phosphonate
1269662-79-4

diethyl ({[4-({3-chloro-4-[(pyridin-2-yl)methoxy]phenyl}amino)-3-cyano-7-ethoxyquinolin-6-yl]carbamoyl}methyl)phosphonate

neratinib
698387-09-6

neratinib

Conditions
Conditions Yield
diethyl ({[4-({3-chloro-4-[(pyridin-2-yl)methoxy]phenyl}amino)-3-cyano-7-ethoxyquinolin-6-yl]carbamoyl}methyl)phosphonate; With sodium ethanolate; lithium chloride; In ethanol; at 0 ℃; for 0.5h;
dimethylaminoacetaldehyde-sodium bisulfite adduct; In ethanol; for 3h;
94.1%
2-(N,N-dimethylamino)ethoxide
52334-92-6

2-(N,N-dimethylamino)ethoxide

diethyl ({[4-({3-chloro-4-[(pyridin-2-yl)methoxy]phenyl}amino)-3-cyano-7-ethoxyquinolin-6-yl]carbamoyl}methyl)phosphonate
1269662-79-4

diethyl ({[4-({3-chloro-4-[(pyridin-2-yl)methoxy]phenyl}amino)-3-cyano-7-ethoxyquinolin-6-yl]carbamoyl}methyl)phosphonate

neratinib
698387-09-6

neratinib

Conditions
Conditions Yield
diethyl ({[4-({3-chloro-4-[(pyridin-2-yl)methoxy]phenyl}amino)-3-cyano-7-ethoxyquinolin-6-yl]carbamoyl}methyl)phosphonate; With sodium ethanolate; lithium chloride; In ethanol; at -5 ℃; for 0.5h;
2-(N,N-dimethylamino)ethoxide; In ethanol; for 0.666667h; Temperature; Solvent; Reagent/catalyst;
95.9%
6-amino-4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]-7-ethoxyquinoline-3-carbonitrile
848139-78-6

6-amino-4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]-7-ethoxyquinoline-3-carbonitrile

(2E)-4-(dimethylamino)but-2-enoic acid hydrochloride
1130155-48-4

(2E)-4-(dimethylamino)but-2-enoic acid hydrochloride

neratinib
698387-09-6

neratinib

Conditions
Conditions Yield
(2E)-4-(dimethylamino)but-2-enoic acid hydrochloride; With oxalyl dichloride; N,N-dimethyl-formamide; In dichloromethane; at 0 - 5 ℃; Inert atmosphere;
6-amino-4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]-7-ethoxyquinoline-3-carbonitrile; In 1-methyl-pyrrolidin-2-one; dichloromethane; at 10 - 25 ℃;
95%
6-amino-4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]-7-ethoxyquinoline-3-carbonitrile
848139-78-6

6-amino-4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]-7-ethoxyquinoline-3-carbonitrile

4-N,N-dimethylaminocrotonoylchloride Hydrochloride
501332-27-0

4-N,N-dimethylaminocrotonoylchloride Hydrochloride

neratinib
698387-09-6

neratinib

Conditions
Conditions Yield
With sodium hydroxide; In 1-methyl-pyrrolidin-2-one; water; at 10 - 40 ℃; for 15h; Solvent;
98%
4-[4-(2-pyridylmethoxy)-3-chloro]amino-6-amino-3-cyano-7-ethoxyquinoline

4-[4-(2-pyridylmethoxy)-3-chloro]amino-6-amino-3-cyano-7-ethoxyquinoline

(2E)-(N,N-dimethylamino)-2-butenoyl chloride
1056149-69-9

(2E)-(N,N-dimethylamino)-2-butenoyl chloride

neratinib
698387-09-6

neratinib

Conditions
Conditions Yield
4-[4-(2-pyridylmethoxy)-3-chloro]amino-6-amino-3-cyano-7-ethoxyquinoline; (2E)-(N,N-dimethylamino)-2-butenoyl chloride; With 1-methyl-pyrrolidin-2-one; In tetrahydrofuran; for 3 - 16h;
With water; In tetrahydrofuran; at 40 ℃;
With sodium hydroxide; In tetrahydrofuran; water; pH=10 - 11;
80%
6-amino-4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]-7-ethoxyquinoline-3-carbonitrile
848139-78-6

6-amino-4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]-7-ethoxyquinoline-3-carbonitrile

trans-4-dimethylamino crotonic acid chloride hydrochloride salt
1055943-40-2

trans-4-dimethylamino crotonic acid chloride hydrochloride salt

neratinib
698387-09-6

neratinib

Conditions
Conditions Yield
With triethylamine; In tetrahydrofuran; at 0 - 10 ℃; for 1h; Reagent/catalyst; Inert atmosphere;
93%
In 1-methyl-pyrrolidin-2-one; at -25 - -20 ℃; for 5h; Temperature;
86.72%
In tetrahydrofuran; 1-methyl-pyrrolidin-2-one; at 0 - 5 ℃; for 5h; Product distribution / selectivity;
68%
In 1-methyl-pyrrolidin-2-one; acetonitrile; Product distribution / selectivity;
64%
6-amino-4-[[3-chloro-4-(pyridin-2-ylmethoxy)phenyl]amino]-7-ethoxyquinoline-3-carbonitrile; trans-4-dimethylamino crotonic acid chloride hydrochloride salt; In ISOPROPYLAMIDE; at -19 - -14 ℃; Industry scale;
With water; potassium hydroxide; In ISOPROPYLAMIDE; at -7 - 42 ℃; pH=10 - 11; Product distribution / selectivity; Industry scale;
In 1-methyl-pyrrolidin-2-one; at 0 - 20 ℃;
104 g
2-chloro 4-aminophenol
3964-52-1

2-chloro 4-aminophenol

2-chloromethylpyridine hydrochloride
6959-47-3

2-chloromethylpyridine hydrochloride

4-chloro-6-(5-(dimethylamino)-2-oxopent-3-enyl)-7-ethoxyquinoline-3-carbonitrile
848133-88-0

4-chloro-6-(5-(dimethylamino)-2-oxopent-3-enyl)-7-ethoxyquinoline-3-carbonitrile

neratinib
698387-09-6

neratinib

Conditions
Conditions Yield
2-chloro 4-aminophenol; 2-chloromethylpyridine hydrochloride; 4-chloro-6-(5-(dimethylamino)-2-oxopent-3-enyl)-7-ethoxyquinoline-3-carbonitrile; In tetrahydrofuran; at 65 ℃; for 6h; Inert atmosphere;
With potassium carbonate; potassium iodide; In tetrahydrofuran; at 60 ℃; for 16h; Reagent/catalyst; Solvent; Temperature; Inert atmosphere;
82.73%
neratinib maleate

neratinib maleate

neratinib
698387-09-6

neratinib

Conditions
Conditions Yield
With sodium hydroxide; In methanol;
88.7%
With triethylamine; In ethanol; acetonitrile; at 73 ℃;

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  • Hangzhou Hysen Pharma co.,Ltd.
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