- Method for synthesizing benzoxazole through microwave radiation of benzamide compound in water phase
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The invention discloses a method for synthesizing benzoxazole through microwave radiation of a benzamide compound in a water phase. The benzamide compound is added into the water phase under the microwave condition to be subjected to a cyclization reaction for generating the benzoxazole under the alkali condition, and the method for preparing the benzoxazole is environmentally friendly, easy and convenient to operate, safe, low in cost and efficient. Compared with the prior art, the method can be applied to a large number of functional groups, the yield is high, the number of by-products is small, and the method is easy to operate, safe, low in cost and environmentally friendly. (Please see the specifications for the formula).
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Paragraph 0020
(2019/03/08)
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- Synthesis and pharmacological characterization of a new benzoxazole derivative as a potent 5-HT3 receptor agonist
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N-(2-Benzoxazol-2-yl-ethyl)-guanidine hydrochloride (10) was synthesized and pharmacologically tested. This compound showed high affinity for the 5-HT3 receptor (Ki=0.77 nM) and potently triggered the von Bezold-Jarisch reflex (BJR) in rats with an ED50=0.52 μg/kg iv and intrinsic activity next to 1 (i.a.=0.94). This stimulant effect was abolished by pretreatment with the 5-HT3 receptor antagonist granisetron and was subject to a rapid and pronounced tachyphylaxis, due to desensitization of the peripheric cardiac 5-HT3 receptor. Consequently, 10 acts as an in vivo 5-HT3 antagonist inhibiting the BJR responses evoked by submaximal doses of 5-HT with an ID50=5.8 μg/kg iv.
- Lopez-Tudanca, Pedro Luis,Labeaga, Luis,Innerarity, Ana,Alonso-Cires, Luisa,Tapia, Ines,Mosquera, Ramon,Orjales, Aurelio
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p. 2709 - 2714
(2007/10/03)
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