202409-85-6

Basic information

• Product Name: 5-chloro-3-[4-(methylsulfonyl)phenyl]pyridin-2(1H)-one
• Synonyms: 5-chloro-3-[4-(methylsulfonyl)phenyl]pyridin-2(1H)-one
• CAS NO: 202409-85-6
• Molecular Weight: 283.735
• Mol File: 202409-85-6.mol
• Article Data: 5

Chemical Properties

• CAS DataBase Reference: 5-chloro-3-[4-(methylsulfonyl)phenyl]pyridin-2(1H)-one(CAS DataBase Reference)
• NIST Chemistry Reference: 5-chloro-3-[4-(methylsulfonyl)phenyl]pyridin-2(1H)-one(202409-85-6)
• EPA Substance Registry System: 5-chloro-3-[4-(methylsulfonyl)phenyl]pyridin-2(1H)-one(202409-85-6)

Safety Data

• Hazardous Substances Data: 202409-85-6(Hazardous Substances Data)

Upstream product

• 149104-88-1 4-methanesulphonylphenylboronic acid 
• 603143-27-7 (4,4,5,5-tetramethyl-2-[4-(methylsulfonyl)phenyl])-1,3,2-dioxaborolane 
• 4214-79-3 5-chloro-2-pyridinol 
• 1224598-12-2 3-[4-(methylsulfonyl)phenyl]pyridin-2(1H)-one 
• 171774-38-2 N-(3-bromo-5-chloropyridin-2-yl)pyridin-1-ium-1-aminide 
• 202409-80-1 5-chloro-3-(4-methylsulfonylphenyl)-2-pyridinamine 
• 1443542-63-9 N-[5-chloro-3-(4-methylsulfonylphenyl)pyridin-2-yl]pyridin-1-ium-1-aminide 
• 202409-84-5 2-Benzyloxy-5-chloro-3-(4-methylsulfonyl)phenylpyridine 

Downstream Products

• 202409-86-7 2,5-dichloro-3-[4-(methylsulfonyl)phenyl]pyridine 
• 202409-31-2 5-Chloro-3-(4-(methylsulfonyl)phenyl)-2-(3-pyridinyl)pyridine 
• 202409-33-4 etoricoxib 
• 202409-81-2 2-bromo-5-chloro-3-(4-(methylsulfonyl)phenyl)pyridine 

Relevant articles and documents

Preparation technology of etoricoxib and reference substance 5-chloro-3-(4-(methyl sulphonyl)phenyl)-2,3-bipyridine of etoricoxib

The invention discloses a preparation technology of etoricoxib and a reference substance 5-chloro-3-(4-(methyl sulphonyl)phenyl)-2,3-bipyridine of etoricoxib. The preparation technology comprises steps as follows: 5-chloro-2-hydroxypyridine is taken as a raw material and subjected to a substitution reaction, and 5-chloro-3-iodopyridine-2-ol is obtained; 5-chloro-3-iodopyridine-2-ol is subjected to a coupled reaction, and 5-chloro-3-(4-(methyl sulphonyl)phenyl)pyridine-2-ol is obtained; 5-chloro-3-(4-(methyl sulphonyl)phenyl)pyridine-2-ol is subjected to the substitution reaction, and 2-bromo-5-chloro-3-(4-(methyl sulphonyl)phenyl)pyridine is obtained; 2-bromo-5-chloro-3-(4-(methyl sulphonyl)phenyl)pyridine is subjected to the coupled reaction, a target product etoricoxib or the reference substance 5-chloro-3-(4-(methyl sulphonyl)phenyl)-2,3-bipyridine of etoricoxib is obtained, and the total yield can reach 18%. The route is one novel technology for synthesizing etoricoxib or the reference substance 5-chloro-3-(4-(methyl sulphonyl)phenyl)-2,3-bipyridine of etoricoxib, and the blank of a synthesis method of the reference substance 5-chloro-3-(4-(methyl sulphonyl)phenyl)-2,3-bipyridine of etoricoxib in China is filled up accordingly.

Phosphorodiamidate-directed metalation of N -heterocycles using Mg- and Zn-TMP bases

Figure presented The strong directing ability of the N,N,N′,N′- tetramethyldiaminophosphorodiamidate group has been used to achieve selective metalations on various heterocycles such as pyridines, quinolines and quinoxalines with TMP-derived bases like TMPMgCl·LiCl, TMP 2Mg·2LiCl, and TMP2Zn·2MgCl 2·2LiCl. This protocol was applied in the synthesis of etoricoxib, talnetant and a P-selectin inhibitor.

Substituted pyridines as selective cyclooxygenase-2 inhibitors

The invention encompasses the novel compound of Formula I as well as a method of treating COX-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. STR1 The invention also encompasses certain pharmaceutical compositions for treatment of COX-2 mediated diseases comprising compounds of Formula I.