162970-49-2Relevant articles and documents
Carbazole-containing amides and ureas: Discovery of cryptochrome modulators as antihyperglycemic agents
Humphries, Paul S.,Bersot, Ross,Kincaid, John,Mabery, Eric,McCluskie, Kerryn,Park, Timothy,Renner, Travis,Riegler, Erin,Steinfeld, Tod,Turtle, Eric D.,Wei, Zhi-Liang,Willis, Erik
supporting information, p. 293 - 297 (2018/01/04)
A series of novel carbazole-containing amides and ureas were synthesized. A structure–activity relationship study of these compounds led to the identification of potent cryptochrome modulators. Based on the desired pharmacokinetic/pharmacodynamic parameters and the results of efficacy studies in db/db mice, compound 50 was selected for further profiling.
An efficient synthesis of 3,3-difluoro-pyrrolidine hydrochloride starting with 2-chloro-2,2-difluoroacetic acid
Wei, Lulin,Makowski, Teresa M.,Rutherford, Jennifer L.
experimental part, p. 354 - 357 (2012/03/27)
A facile and fluorination-free synthesis of 3,3-difluoropyrrolidine hydrochloride (3), an important synthon in the synthesis of biologically active compounds, is reported. The seven-step synthesis starts from the commercially available 2-chloro-2,2-difluoroacetic acid (1) in a three-step telescoped process that produces crystalline N,N-diethyl-2,2-difluoro-3-hydroxy-4- nitrobutanamide (2). A convenient and high-yielding reductive nitromethylation of 2 followed by a catalytic hydrogenation/cyclization sequence and borane reduction affords 3 in good yield and purity.