81528-38-3Relevant academic research and scientific papers
Substituted diaryl compound and preparation method and application thereof
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Paragraph 0073-0075, (2021/09/15)
The invention relates to the field of medicinal chemistry, in particular to a substituted diaryl compound (I). The preparation method comprises the following steps: medicine preparation and medical application thereof. Test results show that the substituted diaryl compound has a good inhibition effect on human lung cancer (A549), human ovarian cancer (SKOV3), human melanoma (A375) and human colon cancer (LOVO) cells. Formula (I):
A facile and efficient method for synthesis of β-iodocarboxylates from terminal epoxides
Zhu, Ye-Fu,Wei, Bo-Le,Wang, Wen-Qiong,Xuan, Li-Jiang
supporting information, (2019/11/26)
A facile and efficient method has been developed for synthesis of β-iodocarboxylates in the presences of Ph3P/I2. Starting from epoxides, a series of β-iodocarboxylate compounds can be directly obtained in toluene media with excellent yields. Moreover, the method was successfully applied for the late-stage modification of natural products, such as isosteviol and vincamine derivatives, achieving the corresponding β-iodocarboxylates in good yields.
Syntheses of pterocarpenes and coumestans via regioselective cyclodehydration
Nayak, Maloy,Jung, Youngeun,Kim, Ikyon
, p. 8074 - 8087 (2016/09/09)
A highly efficient synthetic route to pterocarpenes and coumestans is described. BCl3-mediated dehydrative cyclization of 1,3-diaryloxyacetones under mild conditions permitted regioselective ring closure to afford 3-((2-iodoaryloxy)methyl)benzo
An improved method for the conversion of oxiranes to thiiranes and the discrimination of their base peaks in EI-MS
Chen, Hsing-Ming,Chen, Po-Yuan,Wang, Chih-Feng,Tsai, Jui-Chi,Wang, Eng-Chi
body text, p. 157 - 168 (2012/10/18)
An efficient method for the conversion of oxiranes to thiiranes by treatment with excess ammonium thiocyanate in aqueous media under reflux or by microwave irradiation is reported. ARKAT-USA, Inc.
Thienopyrimidines as β3-adrenoceptor agonists: Hit-to-lead optimization
Tasler, Stefan,Baumgartner, Roland,Ammendola, Astrid,Schachtner, Josef,Wieber, Tanja,Blisse, Marcus,Rath, Sandra,Zaja, Mirko,Klahn, Philipp,Quotschalla, Udo,Ney, Peter
scheme or table, p. 6108 - 6115 (2010/11/19)
Resulting from a vHTS based on a pharmacophore alignment on known β3-adrenoceptor ligands, an aryloxypropanolamine scaffold comprising a thienopyrimidine moiety was further optimized as a human β3-AR agonist, yielding a lead compound with an excellent cellular activity of EC50 = 20 pM, selectivity over hβ1- and hβ2-adrenoceptors and a promising safety profile.
SUBSTITUTED DIHYDRO AND TETRAHYDRO OXAZOLOPYRIMIDINONES, PREPARATION AND USE THEREOF
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Page/Page column 40, (2010/04/23)
The present invention relates to a series of substituted dihydro and tetrahydro oxazolopyrimidinones, specifically, to a series of 2-substituted-2,3-dihydro-oxazolo[3,2-a]pyrimidin-7-ones and 2-substituted-2,3,5,6-tetra-hydro-oxazolo[3,2-a]pyrimidin-7-ones of formula (I): Wherein p, n, X, Y, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein. This invention also relates to methods of making these compounds including novel intermediates. The compounds of this invention are modulators of metabotropic glutamate receptors (mGluR), particularly, mGluR2 receptor. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic neurodegenerative conditions, psychoses, convulsions, anxiety, depression, migraine, pain, sleep disorders and emesis.
