2235-01-0Relevant articles and documents
Schoenberg et al.
, p. 4667 (1966)
1,3-Dioxane as a scaffold for potent and selective 5-HT1AR agonist with in-vivo anxiolytic, anti-depressant and anti-nociceptive activity
Franchini, Silvia,Sorbi, Claudia,Linciano, Pasquale,Carnevale, Gianluca,Tait, Annalisa,Ronsisvalle, Simone,Buccioni, Michela,Del Bello, Fabio,Cilia, Antonio,Pirona, Lorenza,Denora, Nunzio,Iacobazzi, Rosa Maria,Brasili, Livio
, p. 310 - 325 (2019)
A series of compounds generated by ring expansion/opening and molecular elongation/simplification of the 1,3-dioxolane scaffold were prepared and tested for binding affinity at 5-HT1AR and α1 adrenoceptors. The compounds with greater affinity were selected for further functional studies. N-((2,2-diphenyl-1,3-dioxan-5-yl)methyl)-2-(2-methoxyphenoxy)ethan-1-ammonium hydrogen oxalate (12) emerged as highly potent full agonist at the 5-HT1AR (pKi 5-HT1A = 8.8; pD2 = 9.22, %Emax = 92). The pharmacokinetic data in rats showed that the orally administered 12 has a high biodistribution in the brain compartment. Thus, 12 was further investigated in-vivo, showing an anxiolytic and antidepressant effect. Moreover, in the formalin test, 12 was able to decrease the late response to the noxious stimulus, indicating a potential use in the treatment of chronic pain.
Oshima et al.
, p. 1789 (1977)
Silver-Catalyzed Olefination of Acetals and Ketals with Diazoesters to β-Alkoxyacrylates
Li, Jiawen,Qian, Bo,Huang, Hanmin
supporting information, p. 7090 - 7094 (2018/11/23)
The first silver-catalyzed reaction of acetals or ketals with diazoesters leading to trisubstituted or tetrasubstituted β-alkoxyacrylates is now reported. A broad range of acetals and ketals bearing different substituents is compatible with this protocol and thus provides an attractive approach for the synthesis of complex β-alkoxyacrylates. The power of this method was further demonstrated by the successful synthesis of picoxystrobin, which is one of the most popular agricultural fungicides commercialized by Dupont.
PROCESS FOR THE PREPARATION OF BORONIC ACID INTERMEDIATES
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Page/Page column 39; 47; 48, (2014/12/09)
The present invention relates to an improved process for the preparation of 2- pyrimidine-5-boronic acid of formula (I). or salts or esters thereof.