442910-91-0Relevant articles and documents
Direct Formic Acid Mediated Z-Selective Reductive Coupling of Dienes and Aldehydes
Cooze, Christopher,Dada, Raphael,Lundgren, Rylan J.
supporting information, p. 12246 - 12251 (2019/08/01)
Methods for the addition of unsaturated nucleophiles to carbonyls to generate Z-olefin products remain rare and often require either alkyl borane or zinc reductants, limiting their utility. Demonstrated here is that formic acid mediates the Rh-catalyzed,
INDOLES FOR USE IN INFLUENZA VIRUS INFECTION
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, (2016/04/19)
The invention relates to compounds having the structure of formula (I) which can be used for the treatment of or against influenza infections.
Asymmetric synthesis of a glucagon receptor antagonist via friedel-crafts alkylation of indole with chiral α-phenyl benzyl cation
Chung, John Y. L.,Steinhuebel, Dietrich,Krska, Shane W.,Hartner, Fred W.,Cai, Chaoxian,Rosen, Jonathan,Mancheno, Danny E.,Pei, Tao,Dimichele, Lisa,Ball, Richard G.,Chen, Cheng-Yi,Tan, Lushi,Alorati, Antony D.,Brewer, Sarah E.,Scott, Jeremy P.
supporting information, p. 1832 - 1845 (2013/01/15)
Development of a practical asymmetric synthesis of a glucagon receptor antagonist drug candidate for the treatment of type 2 diabetes is described. The antagonist consists of a 1,1,2,2-tetrasubstituted ethane core substituted with a propyl and three aryl groups including a fluoro-indole. The key steps to construct the ethane core and the two stereogenic centers involved a ketone arylation, an asymmetric hydrogenation via dynamic kinetic resolution, and an anti-selective Friedel-Crafts alkylation of a fluoro-indole with a chiral α-phenyl benzyl cation. We also developed two new efficient syntheses of the fluoro-indole, including an unusual Larock-type indole synthesis and a Sugasawa-heteroannulation route. The described convergent synthesis was used to prepare drug substance in 52% overall yield and 99% ee on multikilogram scales.
CRYSTALLINE POLYMORPHIC FORMS OF AN ANTIDIABETIC COMPOUND
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Page/Page column 20, (2010/08/04)
The present invention relates to polymorphic forms of a compound of formula A: This compound is useful as a glucagon receptor antagonist and serves as a pharmaceutically active ingredient for the treatment of type 2 diabetes and related conditions, such as hyperglycemia, obesity, dyslipidemia, and the metabolic syndrome. Hydrates, hemihydrates, anhydrates and similar polymorphic forms are included.
1-SUBSTITUTED-3- BETA-D-GLUCOPYRANOSYLATED NITROGENOUS HETERO- CYCLIC COMPOUNDS AND MEDICINES CONTAINING THE SAME
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Page/Page column 16, (2008/06/13)
A compound having an SGLT1 and/or SGLT2 inhibitory activity which is usable as an agent for the prevention or treatment of diabetes, postprandial hyperglycemia, impaired glucose tolerance, diabetic complications, obesity, etc. It is a 1-substituted-3-(β-D