400608-30-2Relevant academic research and scientific papers
γ-Carboline synthesis enabled by Rh(iii)-catalysed regioselective C-H annulation
Jiang, Bo,Jia, Jingwen,Sun, Yufei,Wang, Yichun,Zeng, Jing,Bu, Xiubin,Shi, Liangliang,Sun, Xiaoying,Yang, Xiaobo
supporting information, p. 13389 - 13392 (2020/11/10)
A redox-neutral Rh(iii)-catalyzed C-H annulation of indolyl oximes was developed. Relying on the use of various alkynyl silanes as the terminal alkyne surrogates, the reaction exhibited a reverse regioselectivity, thus giving an exclusive and easy way for the synthesis of a wide range of substituent free γ-carbolines at C3 position with high efficiency. Deuterium-labelling experiments and kinetic analysis have preliminarily shed light on the working mode of this catalytic system. This journal is
ALKYNYL-SUBSTITUTED HETEROCYCLIC COMPOUND, PREPARATION METHOD THEREFOR AND MEDICAL USE THEREOF
-
Paragraph 0103; 0106; 0107, (2019/07/23)
The present invention relates to an alkynyl-substituted heterocyclic compound acting as an FGFR inhibitor, a preparation method therefor and a medical use thereof. In particular, the present invention relates to a compound as shown in general formula (I) and a pharmaceutically acceptable salt thereof; a pharmaceutical composition including the compound or a pharmaceutically acceptable salt thereof; a method for treating and/or preventing FGFR-associated diseases, particularly tumors, by using the compound or a pharmaceutically acceptable salt thereof; and a preparation method for the compound or a pharmaceutically acceptable salt thereof. The present invention also relates to the use of the compound or a pharmaceutically acceptable salt thereof, or the pharmaceutical composition including the compound or a pharmaceutically acceptable salt thereof in the preparation of a drug for treating and/or preventing FGFR-associated diseases, particularly tumors, wherein the definition of each substituent group in general formula (I) is the same as that in the description.
Alkynyl-substituted heterocyclic compound, preparation method therefor and medical use therefor for effectively treating and/or preventing FGFR-related diseases such as tumors
-
Page/Page column 28-29, (2020/02/18)
The present invention relates to an alkynyl-substituted heterocyclic compound serving as an FGFR inhibitor, a preparation method therefor and a medical use therefor. In particular, the present invention relates to a compound represented by the general formula (I) and its pharmaceutically acceptable salt, a pharmaceutical composition including the compound or its pharmaceutically acceptable salt, a method for treating and/or preventing FGFR-related diseases, particularly tumors, by using the compound or its pharmaceutically acceptable salt, and a preparation method of the compound or its pharmaceutically acceptable salt. The present invention also relates to an use of the compound or its pharmaceutically acceptable salt, or an pharmaceutical composition including the compound or its pharmaceutically acceptable salt in the preparation of a drug for treating and/or preventing FGFR-related diseases, particularly tumors, wherein the definition of each substituent in the general formula (I) is the same as that in the specification.
Vinylogous Nicholas reactions in the synthesis of bi- and tricyclic cycloheptynedicobalt complexes
Kolodziej, Izabela,Green, James R.
, p. 10852 - 10864 (2015/11/17)
The Lewis acid mediated intramolecular Nicholas reactions of allylic acetate enyne-Co2(CO)6 complexes afford cycloheptenyne-Co2(CO)6 complexes in three manifestations. Electron rich aryl substituted alkyne complexes give tricyclic 6,7,x-benzocycloheptenyne complexes, with x = 5, 6, or 7. Allylsilane substituted complexes afford exo methylene bicyclic x,7-cycloheptenyne complexes (x = 6,7). The allyl acetate function may also be replaced by a benzylic acetate, to afford dibenzocycloheptyne-Co2(CO)6 complexes. Following reductive complexation, the methodology may be applied to the synthesis of the icetexane diterpene carbon framework.
Palladium-catalyzed coupling between aryl halides and trimethylsilylacetylene assisted by dimethylaminotrimethyltin
Cai, Liangzhen,Yang, Dujuan,Sun, Zhonghua,Tao, Xiaochun,Cai, Lisheng,Pike, Victor W.
experimental part, p. 1059 - 1062 (2012/01/04)
Palladium-catalyzed coupling between aryl halides, especially less reactive ones or N-heteroaryls, and trimethylsilylacetylene in the presence of dimethylaminotrimethyltin generated the coupled products in high yields. The reaction does not need CuI and base as auxiliary agents.
ASCORBATE, VITAMIN K3 AND HYDROXYTOLANS IN THE TREATMENT OF CANCER
-
, (2009/01/23)
The combination of compounds of the hydroxytolan family with ascorbate plus naphthoquinone (Vitamin K3; VK3), or a quinone or semiquinone analogue of VK3, kill tumor cells, inhibit tumor growth and development, and treat cancer in subjects in need thereof.
Liquid-Crystalline Octopus Dendrimers: Block Molecules with Unusual Mesophase Morphologies
Gehringer, Lionel,Bourgogne, Cyril,Guillon, Daniel,Donnio, Bertrand
, p. 3856 - 3867 (2007/10/03)
The synthesis and the mesomorphic properties of several new main-chain liquid-crystalline dendrimers, thereafter designated as octopus dendrimers in accordance with their eight sidearms, are reported. In these dendritic systems, the arborescence is ensured by anisotropic segments, acting as branching cells with a double multiplicity, which are incorporated at every node of the dendritic architecture. In such a way, these compounds radically differ from the classical end-functionalized liquid-crystalline dendrimers, the most commonly reported systems. Following our previous report on purely homolithic systems, that is, the building blocks constituting the dendritic matrix are all identical, several heterolithic systems made of different anisotropic blocks have been prepared. The dendritic branches and corresponding dendrimers were synthesized using a modular construction. Polarized optical microscopy and X-ray diffraction studies showed that all of these new octopus dendrimers exhibit either smectic-like or columnar phases with novel morphologies, the nature of the mesophases depending on the number of terminal chains attached to the peripheral groups. The mesomorphism of these heterolithic dendrimers is discussed in terms of their intrinsic architecture and compared to the analogous homolithic octopus systems. Models for the molecular organizations within both the smectic and the columnar phases are proposed on the basis of small Bragg angle X-ray diffraction studies and are supported by molecular modelizations. Moreover, this study showed that the mesophase stability is very sensitive to the nature and to the mutual arrangement (the spatial location) of the mesogenic segments within the dendritic matrix, illustrating the intimate relationships existing between the mesomorphic properties and the molecular architecture of these dendrimers.
Methods for treating subjects infected with a herpes virus or neisseria gonorrheae
-
, (2008/06/13)
The present invention provides a method of inhibiting the formation of infectious herpes virus particles, particularly infectious herpes simplex virus (HSV) particles, in a host cell. The method involves administering an effective amount of a hydroxylated
