14315-15-2Relevant academic research and scientific papers
Enantioselective hydroarylation or hydroalkenylation of benzo[b]thiophene 1,1-dioxides with organoboranes
Hu, Fangdong,Jia, Jie,Li, Ximing,Xia, Ying
supporting information, p. 896 - 901 (2021/02/01)
An efficient protocol for the asymmetric hydroarylation and hydroalkenylation of benzo[b]thiophene 1,1-dioxides with organoboranes has been developed. The combination of a rhodium(I) precatalyst and a chiral diene ligand constitutes the catalytic system, which enables the facile synthesis of 2,3-dihydrobenzo[b]thiophene 1,1-dioxides in good yields with high enantioselectivities. The merging of this asymmetric hydroarylation with the downstream alkylations delivers 2,3-dihydrobenzo[b]thiophene 1,1-dioxides that contain two continuous quaternary stereocenters with high enantioselectivities in a diastereodivergent manner.
Structure-based design, synthesis, and biological evaluation of 1,1-dioxoisothiazole and benzo[b]thiophene-1,1-dioxide derivatives as novel inhibitors of hepatitis C virus NS5B polymerase
Kim, Sun Hee,Tran, Martin T.,Ruebsam, Frank,Xiang, Alan X.,Ayida, Benjamin,McGuire, Helen,Ellis, David,Blazel, Julie,Tran, Chinh V.,Murphy, Douglas E.,Webber, Stephen E.,Zhou, Yuefen,Shah, Amit M.,Tsan, Mei,Showalter, Richard E.,Patel, Rupal,Gobbi, Alberto,LeBrun, Laurie A.,Bartkowski, Darian M.,Nolan, Thomas G.,Norris, Daniel A.,Sergeeva, Maria V.,Kirkovsky, Leo,Zhao, Qiang,Han, Qing,Kissinger, Charles R.
supporting information; scheme or table, p. 4181 - 4185 (2009/04/16)
A novel series of HCV NS5B polymerase inhibitors comprising 1,1-dioxoisothiazoles and benzo[b]thiophene-1,1-dioxides were designed, synthesized, and evaluated. SAR studies guided by structure-based design led to the identification of a number of potent NS
HIV integrase inhibitors
-
Page/Page column 35, (2010/11/27)
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
-
Page/Page column 28, (2010/11/27)
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.
BICYCLIC HETEROCYCLES AS HIV INTEGRASE INHIBITORS
-
Page/Page column 158, (2010/11/27)
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.
Bicyclic heterocycles as HIV integrase inhibitors
-
Page/Page column 69, (2008/06/13)
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.
4-AMINO-PIPERIDINE DERIVATIVES AS MONOAMINE UPTAKE INHIBITORS
-
Page/Page column 51, (2008/06/13)
The present invention provides compounds of formula (I) where n, R1, R2, R3, R4, R5 and Heteroaryl are defined herein. The compounds are inhibitors of the uptake of one or more monoamines selected from serotonin, norepinephrine and dopamine and, as such,
Antidermatophytic action of new 1-naphthylmethyl and benzo[b]thiophen-7- ylmethyl hydrazones related to inhibitors of squalene epoxidase
Auzzas, Luciana,Palomba,Boatto,Manconi,Pau,Becciu,Cerri,Tullio,Roana,Carlone
, p. 483 - 489 (2007/10/03)
Two series of hydrazonic compounds related to main classes of inhibitors of fungal squalene epoxidase (SE) were designed and prepared on the hypothesis of a pharmacophoric model. The antifungal activity of the new compounds was evaluated in vitro against
An improved synthesis of benzo[b]thiophene and its derivatives using modified montmorillonite clay catalysts
Clark,Kirk,Yee
, p. 1936 - 1938 (2007/10/02)
Methods for the preparation of benzothiophene (3) and its derivatives by cyclization of phenylthioacetals (1) over ZnCl2-promoted montmorillonite clay are described. Reactions in solution resulted in only moderate (ca. 50%) yields of 3 and the formation of diphenyl disulfide (4) and uncharacterized products. The production of 4 was explained by coordination of 1 via its oxygen atom to active sites of the catalyst and subsequent bimolecular processes. Good to excellent yields (67-98%) of 3 and its derivatives were obtained using vapor phase techniques at 200-300°C to promote the desired intramolecular cyclizations.
ALKYLATION OF THIOPHENES AND PREPARATION OF BENZOTHIOPHENES USING MODIFIED MONTMORILLONITE CLAY CATALYSTS
Clark, Peter D.,Kirk, Andrew,Mesher, Shaun T.,Yee, James G.K.
, p. 441 - 444 (2007/10/02)
Regioselective benzylation of thiophene and benzothiophene using benzyl chloride and a ZnCl2-promoted montmorillonite catalysts is described.An improved process for the cyclization of (arylthio)acetaldehyde dialkyl acetals to benzothiophenes using the same catalyst is also documented.
