206002-17-7Relevant academic research and scientific papers
7- OR 8-HYDROXY-ISOQUINOLINE AND 7- OR 8-HYDROXY-QUINOLINE DERIVATIVES AS ALPHA-1 -ANTITRYPSIN MODULATORS FOR TREATING ALPHA-1 -ANTITRYPSIN DEFICIENCY (AATD)
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Paragraph 00141-00142; 00233; 00234, (2021/10/11)
7- or 8-hydroxy-isoquinoline and 7- or 8-hydroxy-quinoline derivatives as alpha-l-antitrypsin modulators for treating alpha-l-antitrypsin deficiency (AATD).
BIARYL DERIVATIVES AS YAP/TAZ-TEAD PROTEIN-PROTEIN INTERACTION INHIBITORS
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Page/Page column 104, (2021/09/26)
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; (I) a method for manufacturing said compound, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition comprising said compound.
Atroposelective Synthesis of Axially Chiral 4-Aryl α-Carbolines via N-Heterocyclic Carbene Catalysis
Ma, Rui,Wang, Xiaoxue,Zhang, Qiaoyu,Chen, Lei,Gao, Jian,Feng, Jie,Wei, Donghui,Du, Ding
supporting information, p. 4267 - 4272 (2021/05/26)
The first catalytic asymmetric construction of axially chiral 4-aryl α-carboline skeletons has been accomplished through an N-heterocyclic carbene (NHC)-catalyzed atroposelective formal [3 + 3] annulation of 4-nitrophenyl 3-arylpropiolates with 2-sulfonamidoindolines. The synthetic utility of the title compounds has been demonstrated by the diverse late-stage structural modifications. Density functional theory calculations were also conducted to illuminate the key factors for controlling the origin of the enantioselectivity. This strategy not only provides an efficient pathway to access axially chiral α-carboline atropisomers but also offers a novel catalytic enantioselective mode for the construction of axially chiral heterobiaryls by using NHC-bound alkynyl acylazoliums.
A macrocyclic approach to tetracycline natural products. Investigation of transannular alkylations and Michael additions
Wzorek, Joseph S.,Kn?pfel, Thomas F.,Sapountzis, Ioannis,Evans, David A.
supporting information, p. 5840 - 5843 (2013/02/25)
A new approach to the tetracycline core structure is presented. The pivotal intermediate is identified as macrocycle III. The two interior bonds (C4a-C12a and C5a-C11a) are to be constructed through sequential transannular Michael additions (III-II) and compression-promoted transannular isoxazole alkylations from intermediate II.
Total synthesis of paecilospirone
Yuen, Tsz-Ying,Yang, Sung-Hyun,Brimble, Margaret A.
supporting information; scheme or table, p. 8350 - 8353 (2011/10/31)
Neutrality is the best policy: Key features of the first total synthesis of paecilospirone include an anti-selective, lactate-derived aldol reaction, and a double deallylation/spirocyclization conducted at neutral pH to construct the sensitive hydroxy-substituted benzannulated spiroacetal (see scheme; Bn=benzyl, TBS=tert-butyldimethylsilyl, TES=triethylsilyl).
TRICYCLIC HETEROCYCLIC DERIVATIVES
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Page/Page column 135, (2009/04/25)
The present invention relates to a tricyclic heterocyclic derivative of Formula (I) wherein the variables are as defined in the specification. The present invention further relates to pharmaceutical compositions comprising these compounds and to their use in therapy, in particular for the treatment of serotonin-mediated disorders such as obesity, schizophrenia and cognitive dysfunction.
