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Technology Process of AZD-9291 (Mesylate)

AZD-9291 (Mesylate)

Base Information Edit
  • Chemical Name:AZD-9291 (Mesylate)
  • CAS No.:1421373-66-1
  • Molecular Formula:C28H33N7O2.CH4O3S
  • Molecular Weight:595.723
  • Hs Code.:29339900
  • Mol file:1421373-66-1.mol
AZD-9291 (Mesylate)

Synonyms:AZD-9291 (Mesylate);N-[2-[[2-(Dimethylamino)ethyl]methylamino]-4-methoxy-5-[[4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl]amino]phenyl]-2-propenamide methanesulfonate (1:1);AZD-9291 mesylate N-[2-[[2-(Dimethylamino)ethyl]methylamino]-4-methoxy-5-[[4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl]amino]phenyl]-2-propenamide methanesulfonate (1:1);Osimertinib mesylate;Mereletinib mesylate;Osimertinib;N-[2-(2-dimethylaminoethylmethylamino)-4-methoxy-5-[[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino]phenyl]prop-2-enamide mesylate salt;Osimertinib Mesylate(AZD9291)

Suppliers and Price of AZD-9291 (Mesylate)
Supply Marketing:Edit
Business phase:
The product has achieved commercial mass production*data from LookChem market partment
Manufacturers and distributors:
  • Manufacture/Brand
  • Chemicals and raw materials
  • Packaging
  • price
  • Usbiological
  • AZD 9291 mesylate
  • 100mg
  • $ 1168.00
  • TRC
  • AZD-9291Mesylate
  • 100mg
  • $ 60.00
  • TRC
  • AZD-9291Mesylate
  • 25mg
  • $ 45.00
  • Medical Isotopes, Inc.
  • AZD-9291mesylate
  • 100 mg
  • $ 490.00
  • J&W Pharmlab
  • Osimertinibmesylate 99%
  • 5g
  • $ 1800.00
  • J&W Pharmlab
  • Osimertinibmesylate 99%
  • 50mg
  • $ 122.00
  • DC Chemicals
  • AZD-9291mesylate(Osimertinib，Mereletinib) >99%
  • 250 mg
  • $ 300.00
  • ChemScene
  • Osimertinibmesylate 99.94%
  • 5mg
  • $ 60.00
  • ChemScene
  • OsimertinibD6 99.70%
  • 1mg
  • $ 420.00
  • ChemScene
  • Osimertinibmesylate 99.94%
  • 5g
  • $ 580.00
Total 147 raw suppliers
Chemical Property of AZD-9291 (Mesylate) Edit
Chemical Property:
  • PSA：153.79000 
  • LogP:5.81710 
  • Storage Temp.:-20°C Freezer, Under inert atmosphere 
  • Solubility.:DMSO (Slightly), Methanol (Slightly) 
Purity/Quality:

99%min *data from raw suppliers

AZD 9291 mesylate *data from reagent suppliers

Safty Information:
  • Pictogram(s):  
  • Hazard Codes: 
MSDS Files:

SDS file from LookChem

Useful:
  • Description Osimertinib is active against exon 19 deletions, exon 21 mutations, and also the exon 20 T790M mutations. It is preferentially selective for mutated EGFR, and therefore toxicity at therapeutic doses is lower than for first- and second-generation agents. Notably, osimertinib is able to cross the blood-brain barrier, making it active against disease in the CNS.
  • Uses AZD-9291 Mesylate is a potent and selective epidermal growth factor receptor (EGFR) inhibitor.
  • Indications The collection of ibrutinib (Imbruvica(R), Pharmacyclics Inc.), afatinib, and osimertinib represents the small, yet expanding, group of covalent SMKIs. Ibrutinib is a non-receptor Bruton’s tyrosine kinase inhibitor approved for the treatment of relapsed chronic lymphocytic leukemia. Afatinib, approved for NSCLC in 2013 and squamous NSCLC in 2016, is a second-generation irreversible EGFR inhibitor that targets wild-type EGFR, the mutant T790M EGFR, and HER2. Osimertinib (AZD9291), which was approved by FDA in November 2015, is a third-generation irreversible EGFR inhibitor that selectively targets the mutant T790M EGFR. Rociletinib, which shares a high degree of structural similarity with that of osimertinib, is a promising covalent EGFR inhibitor developed by Clovis Oncology aimed for the treatment of patients with EGFR T790M-mutated NSCLC, until the company terminated its development in May 2016 following a negative vote fromthe FDA’sOncologic Drugs Advisory Committee.
Technology Process of AZD-9291 (Mesylate)

There total 21 articles about AZD-9291 (Mesylate) which guide to synthetic route it. The literature collected by LookChem mainly comes from the sharing of users and the free literature resources found by Internet computing technology. We keep the original model of the professional version of literature to make it easier and faster for users to retrieve and use. At the same time, we analyze and calculate the most feasible synthesis route with the highest yield for your reference as below:

synthetic route:

Reference yield: 96.73%

methanesulfonic acid
75-75-2,98527-29-8

methanesulfonic acid

[N-(2-{[2-(dimethylamino)ethyl](methyl)amino}-4-methoxy-5-{[4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl]amino}phenyl)propen-2-amide]
1421373-65-0

[N-(2-{[2-(dimethylamino)ethyl](methyl)amino}-4-methoxy-5-{[4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl]amino}phenyl)propen-2-amide]

N-(2-(N-(2-(dimethylamino)ethyl)-N-methylamino)-4-methoxy-5-((4-(1-methyl-1H-indole-3-yl)pyrimidine-2-yl)amino)phenyl)acrylamide methanesulfonate
1421373-66-1

N-(2-(N-(2-(dimethylamino)ethyl)-N-methylamino)-4-methoxy-5-((4-(1-methyl-1H-indole-3-yl)pyrimidine-2-yl)amino)phenyl)acrylamide methanesulfonate

Guidance literature:
[N-(2-{[2-(dimethylamino)ethyl](methyl)amino}-4-methoxy-5-{[4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl]amino}phenyl)propen-2-amide]; With pyrographite; In acetone; at 25 - 55 ℃;
methanesulfonic acid; at 25 - 55 ℃;

Reference yield: 90.0%

methanesulfonic acid
75-75-2,98527-29-8

methanesulfonic acid

N?2?[[2?(dimethylamino)ethyl]methylamino]?4?methoxy?5?[[4?(1?methyl?1H?indole-3-yl)-2-pyrimidinyl]amino]aniline
1421372-66-8

N?2?[[2?(dimethylamino)ethyl]methylamino]?4?methoxy?5?[[4?(1?methyl?1H?indole-3-yl)-2-pyrimidinyl]amino]aniline

acryloyl chloride
814-68-6,25189-84-8

acryloyl chloride

N-(2-(N-(2-(dimethylamino)ethyl)-N-methylamino)-4-methoxy-5-((4-(1-methyl-1H-indole-3-yl)pyrimidine-2-yl)amino)phenyl)acrylamide methanesulfonate
1421373-66-1

N-(2-(N-(2-(dimethylamino)ethyl)-N-methylamino)-4-methoxy-5-((4-(1-methyl-1H-indole-3-yl)pyrimidine-2-yl)amino)phenyl)acrylamide methanesulfonate

Guidance literature:
N?2?[[2?(dimethylamino)ethyl]methylamino]?4?methoxy?5?[[4?(1?methyl?1H?indole-3-yl)-2-pyrimidinyl]amino]aniline; acryloyl chloride; In dichloromethane; at 0 - 5 ℃; for 2h;
methanesulfonic acid; In dichloromethane; Isopropyl acetate; Reflux;

Reference yield:

3-(2-aminopyrimidin-4-yl)-1-methyl-1H-indole
199865-36-6

3-(2-aminopyrimidin-4-yl)-1-methyl-1H-indole

methanesulfonic acid
75-75-2,98527-29-8

methanesulfonic acid

1-methoxy-2-nitro-5-[(N-(dimethylamino)ethyl)-Ν-methylamino]-4-cinnamamide

1-methoxy-2-nitro-5-[(N-(dimethylamino)ethyl)-Ν-methylamino]-4-cinnamamide

N-(2-(N-(2-(dimethylamino)ethyl)-N-methylamino)-4-methoxy-5-((4-(1-methyl-1H-indole-3-yl)pyrimidine-2-yl)amino)phenyl)acrylamide methanesulfonate
1421373-66-1

N-(2-(N-(2-(dimethylamino)ethyl)-N-methylamino)-4-methoxy-5-((4-(1-methyl-1H-indole-3-yl)pyrimidine-2-yl)amino)phenyl)acrylamide methanesulfonate

Guidance literature:
3-(2-aminopyrimidin-4-yl)-1-methyl-1H-indole; 1-methoxy-2-nitro-5-[(N-(dimethylamino)ethyl)-Ν-methylamino]-4-cinnamamide; With diammonium sulfide; In isopropyl alcohol;
methanesulfonic acid;
upstream raw materials:

4-fluoro-2-methoxy-5-nitro-phenylamine

N?2?[[2?(dimethylamino)ethyl]methylamino]?4?methoxy?5?[[4?(1?methyl?1H?indole-3-yl)-2-pyrimidinyl]amino]aniline

N1-(2-(dimethylamino)ethyl)-5-methoxy-N1-methyl-N4-(4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)-2-nitrobenzene-1,4-diamine

N-(4-fluoro-2-methoxy-5-nitrophenyl)-4-(1-methyl-1H-indole-3-yl)-pyrimidine-2-amine

Refernces Edit

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