268232-16-2Relevant academic research and scientific papers
Ruthenium(II)-Catalyzed Asymmetric Inert C?H Bond Activation Assisted by a Chiral Transient Directing Group
Guo, Weicong,Li, Guozhu,Liu, Qinzhe,Vasamsetty, Laxmaiah,Wang, Jun
supporting information, p. 3475 - 3479 (2020/02/05)
A ruthenium(II)-catalyzed asymmetric intramolecular hydroarylation assisted by a chiral transient directing group has been developed. A series of 2,3-dihydrobenzofurans bearing chiral all-carbon quaternary stereocenters have been prepared in remarkably high yields (up to 98 %) and enantioselectivities (up to >99 % ee). By this methodology, a novel asymmetric total synthesis of CB2 receptor agonist MDA7 has been successfully developed.
Evaluation of the Synthetic Potential of an AHBA Knockout Mutant of the Rifamycin Producer Amycolatopsis mediterranei
Bu?yszko, Ilona,Dr?ger, Gerald,Klenge, Anja,Kirschning, Andreas
supporting information, p. 19231 - 19242 (2016/01/26)
Supplementing an AHBA(-) mutant strain of Amycolatopsis mediterranei, the rifamycin producer, with a series of benzoic acid derivatives yielded new tetraketides containing different phenyl groups. These mutasynthetic studies revealed unique reductive properties of A. mediterranei towards nitro- and azidoarenes, leading to the corresponding anilines. In selected cases, the yields of mutaproducts (fermentation products isolated after feeding bacteria with chemically prepared analogs of natural building blocks) obtained are in a range (up to 118 mg L-1) that renders them useful as chiral building blocks for further synthetic endeavors. The configuration of the stereogenic centers at C6 and C7 was determined to be 6R,7S for one representative tetraketide. Importantly, processing beyond the tetraketide stage is not always blocked when the formation of the bicyclic naphthalene precursor cannot occur. This was proven by formation of a bromo undecaketide, an observation that has implications regarding the evolutionary development of rifamycin biosynthesis.
Elucidation of architectural requirements from a spacer in supported proline-based catalysts of enantioselective aldol reaction
Goren, Kerem,Kehat, Tzofit,Portnoy, Moshe
supporting information; experimental part, p. 59 - 65 (2009/09/06)
In order to delineate the properties of the spacer architecture responsible for the strong positive dendritic effect exhibited by polymer-supported proline-based catalysts, we prepared two series of polystyrene-bound model catalysts. The first series was
NOVEL COMPOUNDS AS AGONIST FOR PPAR GAMMA AND PPAR ALPHA, METHOD FOR PREPARATION OF THE SAME, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME
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Page/Page column 143-144, (2010/11/27)
The present invention relates to novel compounds accelerating the activity of Peroxisome proliferator-activated receptor gamma (PPARγ) and alpha (PPARα), processes of preparing the same, and pharmaceutical compositions containing the same as an active agent.
Molecular tripods showing fluorescence enhancement upon binding to streptavidin
Tae, Woo Kim,Hey, Young Yoon,Park, Jung-Hyun,Kwon, Oh-Hoon,Jang, Du-Jeon,Hong, Jong-In
, p. 111 - 114 (2007/10/03)
(Chemical Equation Presented) We introduce a new approach to biotin-streptavidin assays based on a molecular tripod which consists of biotin, a fluorophore, and a quencher. The interaction between streptavidin and molecular tripods perturbs the ground-state quencher-fluorophore dimeric conformation in the absence of streptavidin and diminishes the intrinsic self-quenching of a quencher-fluorophore pair. The emission intensity of the molecular tripods plus streptavidin is 3.5-5.2 times that of molecular tripods in the absence of streptavidin.
Vitamin D analogues
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Page column 12, (2010/02/05)
The invention concerns novel bi-aromatic compounds having the formula: which are analogs of vitamin D, the process of preparing them, as well as their use in pharmaceutical compositions in human or veterinary medicine, particularly in dermatology, cancer treatment, treatment of auto-immune diseases, and in organ or tissue transplants. Cosmetic compositions and methods of use are also included.
TRICYCLIC DERIVATIVES OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, THEIR PREPARATIONS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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Page 68, (2010/02/10)
The present invention relates to tricyclic derivatives or pharmaceutically acceptable salts thereof, their preparations and pharmaceutical compositions containing them. More precisely, the present invention relates to tricyclic derivatives as colchicine derivatives, pharmaceutically acceptable salts thereof, their preparations and pharmaceutical compositions containing them. Tricyclic derivatives of the present invention show very powerful cytotoxicity to cancer cell lines but were much less toxic than colchicine or taxol, confirmed through animal toxicity test. Tricyclic derivatives of the invention also decrease the volume and weight of a tumor and have a strong angiogenesis inhibiting activity in HUVEC cells. Thus, tricyclic derivatives of the present invention can effectively be used as an anticancer agent, anti-proliferation agent and an angiogenesis inhibitor.
Synthesis and properties of new, spatially relaxed dendrons containing internal carboxyl groups
Kikuzawa, Yoshihiro,Nagata, Toshi
, p. 993 - 1000 (2007/10/03)
We synthesized a series of new dendrons with up to fourteen internal carboxyl groups. These dendrons are made from a branching unit and a spacer unit with a carboxyl group. The growth reactions (formation of the benzylic ether bonds) are completed within
