1133-79-5Relevant articles and documents
Three-Step One-Pot Process of 3-Methyl-5-Benzofuranol from Amine, Aldehydes, and p-Benzoquinone
Liang, Chaoming,Sun, Maolin,Shen, Xinyuan,Shan, Chao,Wang, Weijuan,Cheng, Ruihua,Ye, Jinxing
, p. 810 - 816 (2021)
3-Methyl-5-benzofuranol was prepared by a one-pot process from morpholine, propionaldehyde, and p-benzoquinone in 85-87% isolated yields. Avoiding the tedious multistep isolation and purification operations, this practical and efficient process dramatically enhanced the production efficiency as well as reduced the amount of chemical wastes of reaction. The scale-up results showed that the performance was maintained, suggesting potential large-scale applications. Furthermore, the synthesis strategy showed high efficiency for a wide range of aliphatic aldehydes and ketone derivatives.
Synthesis method of NHTD
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Paragraph 0011; 0039-0042, (2020/07/15)
The invention belongs to the field of medicines, and discloses a synthesis method of NHTD. The synthesis method comprises: (1) carrying out a reaction on a compound I and a compound II to synthesize acompound III; (2) under the condition that zinc halide serves as a catalyst, carrying out a substitution reaction on the compound III and tert-butyl chloride to prepare a compound IV; (3) under the action of an alkali, reacting the compound IV with chloromethyl methyl ether to prepare a compound V; (4) reacting the compound V with n-butyllithium and dimethylformamide to prepare a compound VI; (5)reacting the compound VI under an acidic condition to generate a compound VII; and (6) condensing the compound VII and the compound VIII to obtain a compound IX, namely NHTD. The synthesis method hasthe advantages of cheap and easily available raw materials, mild reaction conditions, short reaction route, high synthesis yield and low environmental pollution, and is suitable for industrial production.
Synthesis and antimycobacterial evaluation of benzofurobenzopyran analogues
Prado, Soizic,Janin, Yves L.,Saint-Joanis, Brigitte,Brodin, Priscille,Michel, Sylvie,Koch, Michel,Cole, Stewart T.,Tillequin, Francois,Bost, Pierre-Etienne
, p. 2177 - 2186 (2008/02/01)
We recently reported that 3,3-dimethyl-3H-benzofuro[3,2,f][1]-benzopyran and its hydrogenated analogue are selective in vitro inhibitors of mycobacterial growth. However, their lack of in vivo activity on a murine model of Mycobacterium tuberculosis infec