75965-66-1Relevant academic research and scientific papers
Synthesis of a radiolabeled charged melatonin receptor ligand
Chu, Guo-Hua,Li, Pui-Kai
, p. 435 - 441 (1998)
The synthesis of the first permanently charged melatonin receptor ligand: N-[2-(2-trimethyl-ammoniumethyleneoxy-7- methoxynaphthyl)ethyl]propionamide iodide (2a, TMEPI) and its Carbon-14 analog (2b, 14C-TMEPI) are described. The ligands can serve as tools to elucidate the mechanism of melatonin receptor regulation. Both compounds 2a and 2b are synthesized in 8 steps. The radiochemical yield and purity of 2b are 99.6 and 99.8% respectively, with specific radioactivity of 716 mCi/mmol.
Design, Synthesis and SAR Studies of Novel and Potent Dipeptidyl Peptidase 4 Inhibitors
Luo, Na,Fang, Xiaoyu,Su, Mingbo,Zhang, Xinwen,Li, Dan,Li, Honglin,Li, Shiliang,Zhao, Zhenjiang
, p. 115 - 120 (2020/12/28)
Dipeptidyl peptidase 4 (DPP-4) is a clinically validated target for the treatment of type 2 diabetes mellitus (T2DM). To discover novel and potent DPP-4 inhibitors, three series of compounds were designed and synthesized in this study based on our previou
Sulfur-containing heterocyclic compound and application thereof as derivative of DPP4 inhibitor
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Paragraph 0072-0075; 0094-0096, (2019/11/12)
The invention relates to a benzo sulfur-containing six-membered ring derivative as a DPP-4 inhibitor and application thereof, in particular to a compound shown in a formula I, a pharmaceutical composition comprising the compound of the formula I and application of the compound to the preparation of a medicament for the treatment of DPP-4 associated diseases or inhibition of DPP-4. Please see the specification for the formula I.
Atropoenantioselective redox-neutral amination of biaryl compounds through borrowing hydrogen and dynamic kinetic resolution
Zhang, Jianwei,Wang, Jian
supporting information, p. 465 - 469 (2017/12/15)
We report herein a novel atropoenantioselective redox-neutral amination of biaryl compounds triggered by a cascade of borrowing hydrogen and dynamic kinetic resolution under the cooperative catalysis of a chiral iridium complex and an achiral Br?nsted acid. This protocol features broad substrate scope and good functional-group tolerance, and allows the rapid assembly of axially chiral biaryl compounds in good to high yields and with high to excellent enantioselectivity.
Atropoenantioselective Redox-Neutral Amination of Biaryl Compounds through Borrowing Hydrogen and Dynamic Kinetic Resolution
Zhang, Jianwei,Wang, Jian
supporting information, p. 465 - 469 (2018/02/21)
We report herein a novel atropoenantioselective redox-neutral amination of biaryl compounds triggered by a cascade of borrowing hydrogen and dynamic kinetic resolution under the cooperative catalysis of a chiral iridium complex and an achiral Br?nsted acid. This protocol features broad substrate scope and good functional-group tolerance, and allows the rapid assembly of axially chiral biaryl compounds in good to high yields and with high to excellent enantioselectivity.
Ruthenium-Catalyzed Atropoenantioselective Synthesis of Axial Biaryls via Reductive Amination and Dynamic Kinetic Resolution
Guo, Donghui,Zhang, Jianwei,Zhang, Bei,Wang, Jian
supporting information, p. 6284 - 6288 (2018/10/05)
The unprecedented ruthenium-catalyzed atropoenantioselective reductive amination of aldehydes with alkylamines via a cascade transfer hydrogenation and dynamic kinetic resolution strategy is described. This protocol features broad substrate scope and good functional group tolerance and allows the rapid assembly of axially chiral biaryls in good to high yields with high to excellent enantioselectivities. In addition, such structural motifs may have potential applications in enantioselective catalysis as chiral ligands or catalysts.
Discovery and Rational Design of Natural-Product-Derived 2-Phenyl-3,4-dihydro-2H-benzo[f]chromen-3-amine Analogs as Novel and Potent Dipeptidyl Peptidase 4 (DPP-4) Inhibitors for the Treatment of Type 2 Diabetes
Li, Shiliang,Xu, Hongling,Cui, Shichao,Wu, Fangshu,Zhang, Youli,Su, Mingbo,Gong, Yinghui,Qiu, Shaobing,Jiao, Qian,Qin, Chun,Shan, Jiwei,Zhang, Ming,Wang, Jiawei,Yin, Qiao,Xu, Minghao,Liu, Xiaofeng,Wang, Rui,Zhu, Lili,Li, Jia,Xu, Yufang,Jiang, Hualiang,Zhao, Zhenjiang,Li, Jingya,Li, Honglin
, p. 6772 - 6790 (2016/08/05)
Starting from the lead isodaphnetin, a natural product inhibitor of DPP-4 discovered through a target fishing docking based approach, a series of novel 2-phenyl-3,4-dihydro-2H-benzo[f]chromen-3-amine derivatives as potent DPP-4 inhibitors are rationally designed utilizing highly efficient 3D molecular similarity based scaffold hopping as well as electrostatic complementary methods. Those ingenious drug design strategies bring us approximate 7400-fold boost in potency. Compounds 22a and 24a are the most potent ones (IC50 ≈ 2.0 nM) with good pharmacokinetic profiles. Compound 22a demonstrated stable pharmacological effect. A 3 mg/kg oral dose provided >80% inhibition of DPP-4 activity within 24 h, which is comparable to the performance of the long-acting control omarigliptin. Moreover, the efficacy of 22a in improving the glucose tolerance is also comparable with omarigliptin. In this study, not only promising DPP-4 inhibitors as long acting antidiabetic that are clinically on demand are identified, but the target fish docking and medicinal chemistry strategies were successfully implemented.
Benzo-hexatomic ring derivative used as DPP-4 inhibitor and application of benzo-hexatomic ring derivative
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, (2016/10/09)
The invention relates to a benzo-hexatomic ring derivative used as a DPP-4 inhibitor and application of the benzo-hexatomic ring derivative, in particular to compounds shown as in formula I, medicine compositions with the compounds shown as in the formula I and application of the compounds in preparing medicines for treating diseases related to DPP-4 or inhibiting the DPP-4.
PROCESS FOR THE SYNTHESIS OF 7-METHOXY-NAPHTHALENE-1-CARBALDEHYDE AND APPLICATION IN THE SYNTHESIS OF AGOMELATINE
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Paragraph 0043; 0044, (2016/11/07)
Process for the industrial synthesis of the compound of formula (I):
Substituted heterocyclic compounds, method for preparing and compositions containing same
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, (2008/06/13)
The invention relates to compounds of formula (I): wherein: R1, R2and R3are as defined in the description, X is as defined in the description, Y represents an oxygen atom, a sulphur atom, a C(H)qgroup, SO or SO2, n is equal to from 0 to 5, A represents a NR5R6group, and medicinal products containing the same which are useful in treating or in preventing melatoninergic disorders.
