98733-09-6Relevant 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.
Synthesis Development of the Selective Estrogen Receptor Degrader (SERD) LSZ102 from a Suzuki Coupling to a C-H Activation Strategy
Baenziger, Markus,Baierl, Marcel,Devanathan, Krishnaswamy,Eswaran, Sumesh,Fu, Peng,Gschwend, Bjoern,Haller, Michael,Kasinathan, Gopu,Kovacic, Nikola,Langlois, Audrey,Li, Yongfeng,Schuerch, Friedrich,Shen, Xiaodong,Wan, Yinbo,Wickendick, Regina,Xie, Siwei,Zhang, Kai
, p. 1405 - 1419 (2020/10/12)
The development of the synthetic process to the selective estrogen receptor degrader (SERD) drug candidate LSZ102 from the medicinal chemistry synthesis to the streamlined large-scale manufacturing route is described. The synthesis of LSZ102 could be sign
Organocatalytic enantioselective tandem sulfa-Michael/aldol reaction to access dihydrothiopyran-fused benzosulfolane skeletons bearing three contiguous stereocenters
Yang, Lei,Zhao, Jian-Qiang,You, Yong,Wang, Zhen-Hua,Yuan, Wei-Cheng
supporting information, p. 12363 - 12366 (2020/10/30)
The first organocatalytic diastereo- and enantioselective tandem sulfa-Michael/aldol reaction of 2-mercaptoindole-3-carbaldehydes and 2-mercaptobenzaldehydes with benzo[b]thiophene sulfones was developed. With multiple hydrogen-bonding thiourea as a catalyst, a wide range of polycyclic dihydrothiopyran-fused benzosulfolanes were smoothly obtained with excellent results (up to 99% yield, 420 : 1 dr and 99% ee) under mild reaction conditions.
SUBSTITUTED TRIAZOLOPYRIDINES HAVING ACTIVITY AS MPS-1 INHIBITORS
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, (2015/01/06)
The present invention relates to substituted triazolopyridine compounds of general formula (I), in which R1, R2, R3, R4, and R5 are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, as well as to intermediate compounds useful in the preparation of said compounds.
NOVEL COMPOUNDS FOR THE TREATMENT OF CANCER
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, (2015/01/09)
The present invention relates to novel compounds showing an inhibitory effect on Mps-1 kinase, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, as well as to intermediate compounds useful in the preparation of said compounds.
Efficient synthesis of 3-oxygenated benzothiophene derivatives
Zhang, Fuyao,Mitchell, David,Pollock, Patrick,Zhang, Tony Y.
, p. 2349 - 2352 (2007/10/03)
An efficient synthesis of 2-bromo-3-aryloxybenzothiophene derivatives by a conjugate addition-elimination sequence of 2,3-dibromo benzothiophene dioxides with phenolic nucleophiles has been developed. These benzothiophene derivatives serve as important in
SELECTIVE ESTROGEN RECEPTOR MODULATORS
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Page/Page column 23-27, (2008/06/13)
The present invention relates to a selective estrogen receptor modulator of formula I: or a pharmaceutical acid addition salt thereof; useful, e.g., for treating endometriosis and uterine leiomyoma.
SELECTIVE ESTROGEN RECEPTOR MODULATORS
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Page/Page column 61-64, (2010/02/13)
The present invention relates to a selective estrogen receptor modulators of formula I (I); or a pharmaceutical acid addition salt thereof; and of formula II (II); or a pharmaceutical salt thereof; useful, e.g., for treating endometriosis and/or uterine leiomyoma/leiomyomata.
Inotropic agents
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, (2008/06/13)
This invention provides for certain imidazo compounds, their pharmaceutical formulations, and their use as positive inotropic agents, bronchodilators, vasodilators, and anticoagulants.
