75104-96-0Relevant academic research and scientific papers
PI3Kalpha selective inhibitor and preparation method and application thereof
-
Paragraph 0099-0101, (2021/08/06)
The invention discloses a PI3Kalpha selective inhibitor and a preparation method and application thereof, a triazine ring benzoxazole compound and a preparation method and application thereof, and the structural formula of the compound is shown as a formula I or a pharmaceutically acceptable salt thereof. Biochemical activity tests show that the compounds have good inhibitory activity on PI3K alpha, so that the compounds can provide effective inhibitors with better selectivity for treatment of diseases regulated by PI3K, and target drugs for treating diseases related to PI3K signal pathways, such as gastric cancer, breast cancer, ovarian cancer and leukemia, are expected to be developed.
CDK6/DYRK2 Double-target inhibitor as well as preparation method and application thereof
-
Paragraph 0047, (2021/02/24)
The present invention discloses a compound represented by the following general formula (I) or a pharmaceutically acceptable salt thereof. The invention also discloses a preparation method of the compound and application of the compound in prevention and/or treatment of cancers or tumor-related diseases, especially breast cancer, prostate cancer, lung cancer, multiple myeloma, leukemia, gastric cancer, ovarian cancer, colon cancer, liver cancer, pancreatic cancer, human glioma and other diseases. The compound provided by the invention is expected to be developed into a new generation of anti-cancer drugs.
Intermediate compound as well as preparation method and application thereof
-
Paragraph 0036; 0043-0045, (2021/07/24)
The invention discloses an intermediate compound as well as a preparation method and application thereof. The synthesized intermediate compound is used for preparing targeted anti-cancer drugs, such as CDK4, CDK6, DYRK2 and other inhibitors, and is used for preventing and/or treating cancers or tumor related diseases including breast cancer, prostate cancer, lung cancer, multiple myeloma, leukemia, gastric cancer, ovarian cancer, colon cancer, liver cancer, pancreatic cancer and human glioma. The intermediate compound is simple in preparation condition, high in reaction yield and stable in performance.
A Mild Synthesis of 2-Substituted Benzothiazoles via Nickel-Catalyzed Intramolecular Oxidative C-H Functionalization
Gao, Ming-Yuan,Li, Jing-Hang,Zhang, Shi-Bo,Chen, Li-Jun,Li, Yue-Sheng,Dong, Zhi-Bing
, p. 493 - 500 (2020/02/04)
A highly efficient synthetic method for the preparation of 2-aminobenzothiazoles starting from arylthioureas has been reported. By using a nickel catalyst, arylthioureas undergo intramolecular oxidative C-H bond functionalization, giving the desired 2-aminobenzothiazoles in good to excellent yields. This protocol features an inexpensive catalyst, low catalyst loading, mild reaction conditions, a short reaction time, and good to excellent yields, and it can be scaled up easily to a gram scale with almost no yields decreasing.
1, 3, 4, 5-TETRAHYDRO-2H-PYRIDO[4,3-B]INDOLE DERIVATIVES FOR THE TREATMENT, ALLEVIATION OR PREVENTION OF DISORDERS ASSOCIATED WITH TAU AGGREGATES LIKE ALZHEIMER'S DISEASE
-
Page/Page column 83; 84, (2019/07/20)
The present invention relates to novel compounds that can be employed in the treatment, alleviation or prevention of a group of disorders and abnormalities associated with Tau (Tubulin associated unit) protein aggregates including, but not limited to, Neurofibrillary Tangles (NFTs), such as Alzheimer's disease (AD).
TETRAHYDROBENZOFURO[2,3-C]PYRIDINE AND BETA-CARBOLINE COMPOUNDS FOR THE TREATMENT, ALLEVIATION OR PREVENTION OF DISORDERS ASSOCIATED WITH TAU AGGREGATES
-
Page/Page column 60-61, (2019/12/28)
The present invention relates to novel compounds of formula (I) that can be employed in the treatment, alleviation or prevention of a group of disorders and abnormalities associated with Tau (Tubulin associated unit) protein aggregates including, but not limited to, Neurofibrillary Tangles (NFTs), such as Alzheimer's disease (AD).
Copper(II)-Promoted Cascade Synthesis of 2-Aminobenzothiazoles Starting from 2-Iodoanilines and Sodium Dithiocarbamates
Zhu, Hui,Zhang, Shi-Bo,Liu, Xing,Cheng, Yu,Peng, Han-Ying,Dong, Zhi-Bing
supporting information, p. 5711 - 5716 (2018/10/31)
A facile and efficient formation of 2-aminobenzothiazoles by a copper(II)-promoted one-pot cascade process was developed. The desired 2-aminobenzothiazoles were synthesized in good to excellent yields (up to 97 %) in the presence of Cu(OAc)2 an
Metal-free or transition-metal-catalyzed one-pot synthesis of 2-aminobenzothiazoles
Xu, Wan,Zeng, Meng-Tian,Liu, Min,Liu, Xing,Chang, Cai-Zhu,Zhu, Hui,Dong, Zhi-Bing
, p. 644 - 654 (2017/10/05)
A series of 2-aminobenzothiazoles were synthesized by using 2-halogen-substituted anilines (halogen = Cl, Br, I) and dithiocarbamates in the presence of KOt-Bu. This simple and efficient protocol lets the reactions undergo in a smooth and rapid way to afford the corresponding 2-aminobenzothiazoles in good yields. It is noteworthy that the present process allows the construction of 2-aminobenzothiazoles from a wide range of 2-halogen-substituted aniline derivatives, including substituted 2-iodoanilines, 2-bromoanilines and 2-chloroanilines.
Palladium-catalyzed tandem synthesis of 2-aminobenzothiazoles starting from unreactive 2-chloroanilines
Xu, Wan,Zeng, Meng-Tian,Liu, Min,Liu, Xing,Chang, Cai-Zhu,Zhu, Hui,Li, Yue-Sheng,Dong, Zhi-Bing
supporting information, p. 641 - 643 (2017/09/01)
A simple and efficient protocol for the synthesis of 2-aminobenzothiazole derivatives is described. 2-Chloroanilines were treated with thiocarbamoyl chloride in the presence of Pd(dba)2 and t-BuOK to afford the corresponding 2-amino-benzothiazoles in good to excellent yield via a tandem manner.
Palladium-Catalyzed Synthesis of 2-Aminobenzothiazoles through Tandem Reaction
Xu, Wan,Zeng, Meng-Tian,Liu, Min,Liu, Sha-Sha,Li, Yue-Sheng,Dong, Zhi-Bing
, p. 3084 - 3090 (2017/07/13)
A variety of 2-aminobenzothiazoles were synthesized by using 2-chloroanilines and dithiocarbamates through a tandem approach in the presence of Pd(PPh 3) 4 and t -BuOK. The facile and efficient protocol enabled the reaction to proceed at a good rate with excellent yields.
