2235-01-0Relevant articles and documents
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.
Practical acetalization and transacetalization of carbonyl compounds catalyzed by recyclable PVP-I
Cao, Fu-Rong,Lu, Guangying,Ren, Jiangmeng,Wang, Di,Zeng, Bu-Bing
, (2021/06/21)
A novel PVP-I catalyzed acetalizations/transacetalizations of carbonyl compounds has been developed processing with a mild and easy handling fashion. Different types of Acyclic and cyclic acetals were prepared from carbonyl compounds or their acetals successfully. Further applications of newly developed catalytic combination were testified. This protocol featured with simplicity of operation, mild reaction condition, short reaction time, recyclable of catalyst and broad substrates scope with excellent yields.
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.
Highly efficient acetalization of carbonyl compounds catalyzed by anilin-aldehyde resin salts
Tanemura, Kiyoshi,Suzuki, Tsuneo
supporting information, p. 797 - 799 (2015/06/22)
A mild procedures for the syntheses of ethylene acetals and dimethyl acetals from the corresponding aldehydes and ketones catalyzed by 1mol% of anilinealdehyde resin salts are described. This method is also useful for the synthesis of dimethyl acetals of diaryl ketones.
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.
PROCESS FOR THE PREPARATION OF BORONIC ACID INTERMEDIATES
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Paragraph 0300-0306, (2014/11/13)
The present invention relates to a process for the preparation of 2-amino-pyrimidine-5-boronic acid of formula (I). or salts or esters thereof.
Process for the preparation of aminoaryl- and aminoheteroaryl boronic acids and esters
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Paragraph 0051-0052, (2014/11/27)
The present invention relates to a process for the preparation of aminoaryl- and aminoheteroaryl boronic acids and esters of formula (I) in high yields The claimed process uses diarylketal formula (V) to generate an arylbromid of formula (III) in which the amino-group is protected as bisarylmethylidenimino-group:
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.
Anodic cleavage of several ketone N-phenylsemicarbazones into methyl N-phenylcarbamate and the corresponding dimethyl acetals
Nishikawa, Shinnosuke,Yamamori, Haruki,Ohashi, Kousuke,Okimoto, Mitsuhiro,Hoshi, Masayuki,Yoshida, Takashi
, p. 1766 - 1771 (2013/05/21)
Several ketone N-phenylsemicarbazones were electrooxidized in the presence of potassium iodide and a base using methanol as the solvent to give nearly commensurate amounts of methyl N-phenylcarbamate and the corresponding dimethyl acetals. Continuous evolution of gaseous nitrogen was observed from the anolyte during the electrooxidation. The reactions were carried out under very mild reaction conditions and are presumed to proceed through a four-electron oxidation process, in which the iodide ion plays an important role as an electron carrier.