206002-17-7Relevant articles and documents
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).
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.
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).