A method for the regioselective synthesis of 1-alkyl-1H-indazoles
A method for the regioselective synthesis of 3-unsubstituted 1-alkyl-1H-indazoles, starting with 2-halobenzonitriles and N-alkylhydrazines, is described. The two-step reaction pathway proceeds through the intermediacy of 1-alkyl-3-amino-1H-indazoles follo
(Chemical Equation Presented) A five-step synthesis of a TRPV1 receptor antagonist 1 is described. The key step involves a novel palladium-catalyzed amidation reaction of 4-chloro-1-methylindazole 8 with the benzyl urea 9 to form the unsymmetrically subst
Yu, Su,Haight, Anthony,Kotecki, Brian,Wang, Lei,Lukin, Kirill,Hill, David R.
experimental part
p. 9539 - 9542
(2010/03/03)
METHODS FOR MAKING CENTRAL NERVOUS SYSTEM AGENTS THAT ARE TRPV1 ANTAGONISTS
The invention discloses compounds of formula ( II ): and methods of making the compounds, which are VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence and bladder overactivity.
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Page/Page column 43-44
(2009/10/22)
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