210346-16-0Relevant articles and documents
PYRAZOLE DERIVATIVES AS SGC STIMULATORS
-
Paragraph 00224, (2016/04/09)
There are described imidazole and pyrazole derivatives which are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds are also useful for treating, preventing or managing various disorders that are herein disclosed.
Asymmetric cyanation of nitroalkenes catalyzed by a salen-titanium catalyst
Lin, Li,Yin, Wen,Fu, Xu,Zhang, Jinlong,Ma, Xiaojuan,Wang, Rui
, p. 83 - 89 (2012/01/14)
The salen-Ti complex catalyzed cyanation of nitroolefins was accomplished via the silyl nitronate intermediate for the synthesis of chiral β-nitronitriles with e.r. up to 92:8 and high yields (up to 90%). The catalyst also kept a high turnover frequency a
Enantioselective Friedel-Crafts reactions between phenols and N-tosylaldimines catalyzed by a leucine-derived bifunctional catalyst
Li, Guo-Xing,Qu, Jin
supporting information; experimental part, p. 5518 - 5520 (2012/07/01)
Enantioselective Friedel-Crafts reactions between phenols and N-tosylaldimines were developed using a bifunctional catalyst readily prepared from l-leucine. The chiral benzylic amine products were obtained in high yields (up to 96% yield) and good to high enantiomeric excesses (up to 95% ee).
Practical synthesis of enantiomerically pure β2-amino acids via proline-catalyzed diastereoselective aminomethylation of aldehydes
Chi, Yonggui,English, Emily P.,Pomerantz, William C.,Horne, W. Seth,Joyce, Leo A.,Alexander, Lane R.,Fleming, William S.,Hopkins, Elizabeth A.,Gellman, Samuel H.
, p. 6050 - 6055 (2008/02/08)
Proline-catalyzed diastereoselective aminomethylation of aldehydes using a chiral iminium ion, generated from a readily prepared precursor, provides α-substituted-β-amino aldehydes with 85:15 to 90: 10 dr. The α-substituted-β-amino aldehydes can be reduce
New scalable asymmetric aminomethylation reaction for the synthesis of β2-amino acids
Moumne, Roba,Denise, Bernard,Guitot, Karine,Rudler, Henri,Lavielle, Solange,Karoyan, Philippe
, p. 1912 - 1920 (2008/02/06)
β-Amino acids are useful tools in the design of peptidomimetics, and the development of new methods for their syntheses, particularly the synthesis of β2-amino acids, remains an important challenge. Here we report a new scalable route based on the aminomethylation of silyl ketene N,O-acetals by Mannich-type iminium electrophiles. Wiley-VCH Verlag GmbH & Co. KGaA, 2007.
CONCISE BETA2-AMINO ACID SYNTHESIS VIA ORGANOCATALYTIC AMINOMETHYLATION
-
Page/Page column 14; 32; 39; 42-43; 47, (2010/11/28)
The present invention provides a method for the synthesis of ?2-amino acids. The method also provides methods yielding a-substituted ?-amino aldehydes and ?-substituted γ-amino alcohols. The present method according to this invention allows for increased yield and easier purification using minimal chromatography or crystallization. The methods described herein are based on an aldehyde aminomethylation which involves a Mannich reaction between an aldehyde and a formaldehyde-derived N,O-acetal (iminium precursor) and a catalyst, such as, for example, L-proline or a pyrrolidine. The invention allows for large scale, commercial preparation of ?2-amino acids.