49827-15-8Relevant articles and documents
Synthesis and biological evaluation of a water-soluble derivative of the potent V-ATPase inhibitor archazolid
Persch, Elke,Basile, Teodora,Bockelmann, Svenja,Huss, Markus,Wieczorek, Helmut,Carlomagno, Teresa,Menche, Dirk
, p. 7735 - 7738 (2012)
The water-solubility of the highly potent V-ATPase inhibitors archazolid A and the glucosylated derivative archazolid C was studied in the presence of a wide range of cosolvents, revealing very low solubilites. The first water-soluble analogue was then designed, synthesized, and evaluated for V-ATPase inhibitory activity in vitro.
Synthesis of Kainoids and C4 Derivatives
Tian, Zhenlin,Menard, Frederic
, p. 6162 - 6170 (2018/05/23)
A unified stereoselective synthesis of 4-substituted kainoids is reported. Four kainic acid analogues were obtained in 8-11 steps with up to 54% overall yields. Starting from trans-4-hydroxy-l-proline, the sequence enables a late-stage modification of C4 substituents with sp2 nucleophiles. Stereoselective steps include a cerium-promoted nucleophilic addition and a palladium-catalyzed reduction. A 10-step route to acid 21a was also established to enable ready functionalization of the C4 position.
Δ3 Asymmetric synthesis method -2 - hydroxyl psoralen and analogue compound
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Paragraph 0029-0031, (2016/11/07)
The invention belongs to the field of chemical synthesis, provides a novel method for synthesizing delta3-2-hydroxybakuchiol and particularly relates to an asymmetric synthesis method for delta3-2-hydroxybakuchiol and analog compounds. The delta3-2-hydroxybakuchiol and the analog compounds, the general formula of which is (I), are synthesized by an asymmetric synthesis route. Problems in the prior art, that the content of the delta3-2-hydroxybakuchiol obtained by extraction and separation from plants is very low, an extraction rate is very low, the delta3-2-hydroxybakuchiol is prone to oxidative deterioration in extraction and separation processes, and the like, are overcome by the method. The method can provide sufficient samples for related pharmaceutical research, and provides good foundations for pharmaceutical research on antibiosis, infection resistance, oxidation resistance, pigment deposition resistance, reduction of bone loss, immunosuppression, liver damage, sedation and hypnosis, and the like. In the formula (I), R1 is selected from 4-hydroxy, 3-hydroxy, 2-hydroxy, hydrogen, 4-methyl, 4-methoxy, 4-trifluoromethyl, 3,4-[d][1,3]dioxole, and 3,4-phenyl; R2 is selected from methyl, ethyl, and butyl; and R3 is selected from vinyl, ethyl and cyclopropyl.
