410545-73-2

Upstream product

• 410545-72-1 2-(bromomethyl)-5-fluoro-N,N-dimethylbenzenesulfonamide 
• 445-05-6 5-fluoro-2-methylbenzenesulfonyl chloride 
• 410545-71-0 5-fluoro-N,N,2-trimethylbenzenesulfonamide 

Downstream Products

• 410545-74-3 2-(aminomethyl)-5-fluoro-N,N-dimethylbenzenesulfonamide 
• 869591-74-2 2-(aminomethyl)-5-fluoro-N,N-dimethylbenzenesulfonamide hydrochloride 

Relevant academic research and scientific papers

Practical synthesis of 4-fluoro-2-(methylthio)benzylamine and the corresponding sulfone and sulfonamide

Practical syntheses of 4-fluoro-2-(methylthio)benzylamine 1 and the corresponding 2-methylsulfonyl analog 2 are reported. The methylthio moiety was introduced regioselectively by two methods. In the first method, metallation of 4-fluoro-2-bromobenzoic acid, followed by treatment with dimethyl disulfide resulted in an easily isolated intermediate, which was suitable for further elaboration to the benzylamine 1. In the second method, selective nucleophilic aromatic substitution of 2,4-difluorobenzonitrile with methanethiolate was explored, and a mechanistic rationale was offered for solvent effects on regioselectivity. Optimized conditions furnished the key 4-fluoro-2-(methylthio) benzonitrile for further functionalization to the 2-methylsulfonyl-4- fluorobenzylamine 2. In addition, the analogous sulfonamide 3 was prepared in a straightforward manner from 5-fluoro-2-methylbenzenesulfonyl chloride. Copyright Taylor & Francis Group, LLC.

HIV integrase inhibitors

The invention encompasses a series bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.

HIV INTEGRASE INHIBITORS

The invention encompasses a series bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.

HIV INTEGRASE INHIBITORS: CYCLIC PYRIMIDINONE COMPOUNDS

The invention encompasses a series of pyrimidinone compounds which inhibit HIV integrase and thereby prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses intermediates useful for making the pyrimidone compounds. Additionally, pharmaceutical compositions and methods for treating those infected with HIV are encompassed. Formula: (I).

BICYCLIC HETEROCYCLES AS HIV INTEGRASE INHIBITORS

The invention encompasses a series cyclic bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.

HIV integrase inhibitors: cyclic pyrimidinone compounds

The invention encompasses a series of pyrimidinone compounds which inhibit HIV integrase and thereby prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses intermediates useful for making the pyrimidone compounds. Additionally, pharmaceutical compositions and methods for treating those infected with HIV are encompassed.

Bicyclic heterocycles as HIV integrase inhibitors

The invention encompasses a series cyclic bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.

Aza- and polyaza-naphthalenyl carboxamides useful as HIV integrase inhibitors

Aza- and polyaza-naphthalenyl carboxamide derivatives including certain quinoline carboxamide and naphthyridine carboxamide derivatives are described. These compounds are inhibitors of HIV integrase and inhibitors of HIV replication, and are useful in the