171230-81-2Relevant articles and documents
Divergent total synthesis of aspinolides B, E and J
Chang, Caizhu,Geng, Jialin,Du, Yuguo,Lv, Qingwei,Dong, ZhiBing,Liu, Jun
, p. 3933 - 3938 (2019)
Stereoselective total synthesis of aspinolides B, E and J, naturally occurring 10-membered lactones, were accomplished by divergent strategies starting from the commercially available 2,3-O-isopropylidene-D-ribose and methyl D-lactate. The synthesis features rapid access to the both key fragments from chiral pool and the formation of 10-membered ring lactones containing trans double bond employing cross-metathesis reaction (CM) and intramolecular Shiina macrolactonization.
Determination of the absolute configuration of the diterpene tonantzitlolone B
Busch, Torsten,Schuster, Hannah,Kirschning, Andreas
, p. 5273 - 5275 (2008)
In this work synthetic and semi-synthetic studies toward the antitumor active natural product tonantzitlolone B are described, starting with an advanced intermediate obtained from the total synthesis of tonantzitlolone and a natural sample of this compound, respectively. The unknown absolute configuration of the stereogenic center in the side chain was elucidated to be (R).
Structure–activity relationship study of the anti-obesity natural product yoshinone A
Kawazoe, Yoshinori,Itakura, Yuki,Inuzuka, Toshiyasu,Omura, Sachikazu,Uemura, Daisuke
, p. 226 - 232 (2021/03/06)
Yoshinone A was derived from marine algae and shown to inhibit adipogenic differentiation. The natural compound is composed of a γ-pyrone ring and a side chain and that contains two asymmetric carbons. Although their absolute configuration has been determ
CYCLIC COMPOUNDS AND METHODS OF USING SAME
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Page/Page column 326, (2021/07/02)
The present application relates to compounds of Formula (I), as defined herein, and pharmaceutically acceptable salts thereof which are MALT1 inhibitors. The present application also describes pharmaceutical composition comprising a compound of Formula (I), and pharmaceutically acceptable salts thereof, and methods of using the compounds and compositions for treating diseases, such as cancer, autoimmune disorders, and inflammatory disorders.
C11-CYCLIC SUBSTITUTED 13-MEMBERED MACROLIDES AND USES THEREOF
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Paragraph 00346, (2020/06/10)
Provided are 13-membered macrolides for the treatment of infectious diseases. The 13- membered macrolides described herein are azaketolides. Also provided are methods for preparing the 13-membered macrolides, pharmaceutical compositions comprising the 13-
Stereoselective Total Synthesis of (+)-Aristolactam GI
Luong, Tuan M.,Pilkington, Lisa I.,Barker, David
, p. 5747 - 5756 (2019/05/10)
Aristolactams are an important subgroup of aporphinoids, which all share a common phenanthrene chromophore motif that is thought to be responsible for the range of interesting physicochemical and biological properties exhibited by these compounds. Among all of the aristolactams discovered, (+)-aristolactam GI displays a unique structural feature of having the aristolactam scaffold linked via a benzodioxane ring to a phenyl propanoid unit, resulting in the compound being an aporphinoid-lignan hybrid. The synthesis of (+)-aristolactam GI was achieved first by synthesis of an orthogonally protected aristolactam, which was prepared using a Suzuki/aldol cascade to convert a differentially protected isoindolin-1-one to the required phenanthrene. The required enantiopure phenyl propanoid unit was prepared from readily available (R)-methyl lactate. A selective Mitsunobu reaction was used to combine these two key fragments, prior to the formation of the linking benzodioxane in the final step. The absolute stereochemistry of the natural product was confirmed to be 7′S, 8′S.
COMPOUNDS, COMPOSITIONS AND METHODS FOR INCREASING CFTR ACTIVITY
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Paragraph 0107, (2019/04/27)
The present disclosure features methods of treating a condition associated with decreased CFTR activity or a condition associated with a dysfunction of proteostasis comprising administering to a subject an effective amount of compounds disclosed herein.
Chiron approach towards optically pure γ-valerolactone from alanine
Datrika, Rajender,Kallam, Srinivasa Reddy,Katta, Rambabu,Siddaiah, Vidavalur,Pratap
supporting information, p. 2801 - 2808 (2018/12/04)
A concise synthesis of both enantiomers of γ-valerolactone has been developed from commercially available Alanine. The key steps in the synthesis of these γ-Lactones are DIBAL-H reduction of ester (9) followed by in situ Wittig reaction with EtO2CCH = PPh3 ylide (13) (Z/E = 1: 3.5) and one pot lactonization triggered by deprotection of O-TBS ether (14).
2,5-DISUBSTITUTED 3-METHYL PYRAZINES AND 2,5,6-TRISUBSTITUTED 3-METHYL PYRAZINES AS ALLOSTERIC SHP2 INHIBITORS
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Paragraph 0672, (2018/03/26)
The present disclosure is directed to inhibitors of SHP2 and their use in the treatment of disease. Also disclosed are pharmaceutical compositions comprising the same.
COMPOUNDS, COMPOSITIONS AND METHODS OF INCREASING CFTR ACTIVITY
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Paragraph 0124, (2017/02/24)
The present disclosure features compounds such as those having the Formulae (I) and (II), which can increase cystic fibrosis transmembrane conductance regulator (CFTR) activity as measured in human bronchial epithelial (hBE) cells. The present disclosure also features methods of treating a condition associated with decreased CFTR activity or a condition associated with a dysfunction of proteostasis comprising administering to a subject an effective amount of a disclosed compound, such as a compound of Formula (I) or (II).
