51026-98-3Relevant academic research and scientific papers
Ti(iv)-catalyzed cascade synthesis of tetrahydrofuro[3,2-d]oxazole from arene-1,4-diones
Li, Gang,Li, Li,Huang, Haihong,Yin, Dali
, p. 4418 - 4421 (2015)
A tetrahydrofuro[3,2-d]oxazole scaffold was synthesized efficiently and stereoselectively. The tandem ionic hydrogenation, ketalization, and intramolecular cyclization of arene-1,4-diones with a combination of TiCl4/Et3SiH give facile access to tetrahydrofuro[3,2-d]oxazole derivatives in good yields at room temperature.
Nitro-acetic acid ethyl ester and intermediate preparation method (by machine translation)
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Paragraph 0037-0050, (2017/11/16)
The invention discloses a nitro-acetic acid ethyl ester and intermediate preparation method. 2 - nitro-acetyl-acetic acid ethyl ester preparation method, comprises the following steps: the acetyl ethyl acetate and through activating the nitric acid reagent from different pipeline entering the micro-channel reactor, the reaction is carried out; wherein the reaction temperature is 5 - 50 °C. By using micro-channel reactor preparing nitro-acetic acid ethyl ester, not only can greatly shorten the reaction time, to enhance the efficiency of the reaction, but also can reduce the generation of by-products, the security is increased, the production cost is reduced, can be suitable for industrial production. (by machine translation)
Synthesis of α-functional nitro compounds by the nitration of activated carbonyl compounds in a two-phase system
Kislyi, V. P.,Laikhter, A. L.,Ugrak, B. I.,Semenov, V. V.
, p. 70 - 74 (2007/10/02)
2-Nitro-1,3-dicarbonyl and α-nitromonocarbonyl compounds were synthesized in the yields variyng from moderate (30percent) to nearly quantitative by the nitration of β-dicarbonyl compounds in a two-phase system: sulfuric/nitric acid mixture - chloroform at -10 - 10 deg C.The use of phase transfer conditions made it possible to avoid the formation of furoxans as by-products and to simplify the isolation of products.This method is quite common for preparing various α-functional nitro compounds including those containing a CF3-group. - Key words: nitration, α-functional nitro compounds.
Bromobenzofuran-based non-peptide antagonists of angiotensin II: GR138950, a potent antihypertensive agent with high oral bioavailability
Judd,Dowle,Middlemiss,Scopes,Ross,Jack,Pass,Tranquillini,Hobson,Panchal,Stuart,Paton,Hubbard,Hilditch,Drew,Robertson,Clark,Travers,Hunt,et al.
, p. 3108 - 3120 (2007/10/02)
We have identified GR138950, a potent antagonist of the angiotensin II receptor with high oral bioavailability, as our second drug candidate to GR117289. Using GR117289, a compound with moderate bioavailability (20%) in man as a lead, we pursued a strategy aimed at enhancing bioavailability. The strategy was based on SAR established around the diacid GR117289, and from this, it was proposed that a monoacid, in particular a trifluoromethanesulfonamide, should be better absorbed after oral administration and have enhanced oral bioavailability. This led to the identification of GR138950, a potent antihypertensive agent in the renal hypertensive rat, causing sustained falls in blood pressure after oral administration. Oral bioavailability of GR138950 in rats and dogs is high, confirming that GR138950 is well absorbed after oral administration. Moreover, the low plasma clearance and long plasma half-life suggest that this compound will be suitable for once a day administration. Furthermore, the preliminary data indicate that the high bioavailability of GR138950 seen in rats and dogs translates to man. These results demonstrate clearly that GR138950 has the potential to be a clinically effective antihypertensive agent. Further studies are in progress to evaluate GR138950 in the treatment of hypertension.
