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.
The mukaiyama aldol reactions for congested ketones catalyzed by solid acid of tin(IV) ion-exchanged montmorillonite
Takehira, Satoshi,Masui, Yoichi,Onaka, Makoto
supporting information, p. 498 - 500 (2014/04/17)
Tin(IV) ion-exchanged montmorillonite (Sn-Mont) was found to be an excellent solid acid catalyst for the Mukaiyama aldol reactions of congested ketones with silicon enolates from ketones as well as esters. It was disclosed that Sn-Mont was far more active than other metal ion-or proton-exchanged montmorillonites and typical homogeneous acid catalysts such as TMSOTf and BF3?OEt2.