52727-44-3Relevant academic research and scientific papers
Ketoserin intermediate and preparation method of ketoserin
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, (2021/01/15)
The invention discloses a preparation method of a ketoserin intermediate 2, 3-dihydro-5H-oxazolo[2, 3-B]quinazoline-5-ketone and a preparation method of ketoserin, and the reaction equation of the preparation method of the ketoserin intermediate 2, 3-dihydro-5H-oxazolo[2, 3-B]quinazoline-5-ketone is shown in the specification: in the reaction, sodium carbonate and acetonitrile are used, no catalyst is added, inorganic salt is removed through hot filtration after the reaction, filtrate is evaporated to dryness, acetonitrile is recycled, and an intermediate 04, namely the ketoserin intermediate2, 3-dihydro-5H-oxazolo[2, 3-B]quinazoline-5-ketone, is obtained. The method is simple and convenient to operate, lower in cost, better in product character and more beneficial to synthesis of a finalproduct.
Synthesis and Discovery of Arylpiperidinylquinazolines: New Inhibitors of the Vesicular Monoamine Transporter
Provencher, Brian A.,Eshleman, Amy J.,Johnson, Robert A.,Shi, Xiao,Kryatova, Olga,Nelson, Jared,Tian, Jianhua,Gonzalez, Mario,Meltzer, Peter C.,Janowsky, Aaron
supporting information, p. 9121 - 9131 (2018/10/20)
Methamphetamine, a human vesicular monoamine transporter 2 (VMAT2) substrate, releases dopamine, serotonin, and norepinephrine from vesicles into the cytosol of presynaptic neurons and induces reverse transport by the monoamine transporters to increase ex
VMAT INHIBITORY COMPOUNDS
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Paragraph 0122-0123, (2016/04/01)
Disclosed herein are compounds that bind to the vesicular monoamine transporter 2 (VMAT2), pharmaceutical compositions comprising those compounds, and methods of treatment using said compounds and pharmaceutical compositions.
A new and rapid access to homochiral 2,3-dihydro-oxazolo[2,3-b]quinazolin-5-ones
Gueyrard, David,Leoni, Onofrio,Palmieri, Sandro,Rollin, Patrick
, p. 337 - 340 (2007/10/03)
Starting from homochiral 1,3-oxazolidine-2-thiones 1, a two-step sequence led to homotopic 2,3-dihydro-oxazolo[2,3-b]quinazolin-5-one derivatives 3. The sequence was developed and studied regarding its scope and limitations.
Reactions of Anthranilamide with Isocyanates: A New Facile Synthesis of 2,3-Dihydro-5H-oxazoloquinazolin-5-one and 3,4-dihydro-2H,6H-oxazinoquinazolin-6-one
Chern, Ji-Wang,Shish, Fang-Jy,Chang, Chau-Dung,Chan, Chao-Han,Liu, Kang-Chien
, p. 1103 - 1105 (2007/10/02)
2,3-Dihydro-5H-oxazoloquinazolin-5-one 5a was synthesized from anthranilamide 1 and 2-chloroethyl isocyanate either by a direct reflux in methanol, or by stirring at room temperature in acetonitrile leading to the intermediate, 2-(2-chloroethyl ureido)benzamide 6a which was subsequently cyclized on heating with an organic base.However, when compound 6a was refluxed with concentrated hydrochloric acid, it furnished 3-(2-chloroethyl)-2,4-dioxo-1H,3H-quinazoline 2a in a good yields. 3,4-Dihydro-2H,6H-oxazinoquinazolin-6-one 5b, 3-(3-chloropropyl)-2,4-dioxo-1H,3H-quinazoline 2b and 2-(3-chloropropyl ureido)benzamide 6b were obtained similarly from 1 and 3-chloropropyl isocyanate.
Reactions of o-Aminonitriles with Isocyanates. 1. A Two-Step Synthesis of 2,6-Dihydroimidazoquinazolin-5-(3H)one
Papadopoulos, Eleftherios Paul
, p. 1553 - 1558 (2007/10/02)
The reaction of anthranilonitrile with 2-chloroethyl isocyanate yields 2-benzonitrile (6) which, upon heating, or treatment with base, undergoes a double cyclization to form 2,6-dihydroimidazoquinazolin-5-(3H)one (8) in excellent yield.When heated with hydrochloric acid, 6 is converted initially into 2-(2-chloroethylamino)-4H-benzoxazin-4-one (18) and further into 3-(2-chloroethyl)-2,4-(1H,3H)quinazolinedione (15).The acid-catalyzed reaction of 2,3-dihydro-5H-oxazoloquinazolin-5-one (14) with nucleophilic reagents yields 3-substituted 2,4-(1H,3H)quinazolinediones.
