Retention of chirality of 5-membered alicyclic α-amino acids bearing N-(2-phenyl)benzoyl group in photoinduced decarboxylative intermolecular radical addition to acrylonitrile
Photoinduced decarboxylative radical additions of 5-membered alicyclic α-amino acids bearing a (2-phenyl)benzoyl protective group to acrylonitrile under mild organic photoredox catalysis conditions furnished γ-amino acid derivatives with high retention of chirality via the memory of chirality (MOC) strategy. The retention of chirality in the photoinduced decarboxylation was strongly dependent on the structure of the alicyclic α-amino acids and alkenes. To the best of our knowledge, this is the first example of the decarboxylative intermolecular radical addition to alkenes with retention of chirality at the position of radical generation using the MOC strategy.
Copper-catalyzed intramolecular N-arylation of quinazolinones: Facile convergent approach to (-)-circumdatins H and J
A copper-catalyzed intramolecular N-arylation of a quinazolinone nucleus that furnished the central benzodiazepine core unit has been demonstrated to accomplish an efficient convergent total synthesis of (-)-circumdatins H and J.
Kshirsagar, Umesh A.,Argade, Narshinha P.
supporting information; experimental part
p. 3716 - 3719
(2010/11/04)
AMIDE DERIVATIVES AND THEIR USE AS CHLORIDE CHANNEL BLOCKERS
The present invention relates to novel amide derivatives useful as chloride channel blockers. In other aspects the invention relates to the use of these compounds in a method for therapy, such as for the treatment of bone metabolic diseases, diseases resp
The association of ICAM-1 with LFA-1 plays a critical role in several autoimmune diseases. N-2-Bromobenzoyl L-tryptophan, compound 1, was identified as an inhibitor to the formation of the LFA-1/ICAM complex. The SAR of the amino acid indicates that the carboxylic acid is required for inhibition and that L-histidine is the most favored amino acid.
Burdick, Daniel J.,Paris, Ken,Weese, Kenneth,Stanley, Mark,Beresini, Maureen,Clark, Kevin,McDowell, Robert S.,Marsters Jr., James C.,Gadek, Thomas R.
p. 1015 - 1018
(2007/10/03)
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