- Synthetic method of alicyclic diester
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The invention discloses a synthetic method of alicyclic diester. The synthetic method comprises the following steps: enabling diacid comprising a multi-carbon lipid chain end group or diester containing a multi-carbon lipid chain end group to react with a first halogenation reagent, after the reaction is completed, adding a second halogenation reagent into a reaction product, after the reaction iscompleted, re-esterifying, and obtaining the di-ester of di-halogenation; adding the di-ester of the di-halogenation into an organic solvent, adding alkali to perform the reaction, after the reactionis completed, adding acid to perform the neutralization, and obtaining annular di-ester; and performing the reduction reaction for the annular di-ester, and obtaining the alicyclic diester. By adopting the synthetic method, a novel reaction path is developed, and the direct-chain end-group diacid or diester is used as a raw material to prepare the alicyclic diester by virtue of bromination reaction, ring-closing reaction and the reduction reaction. The initial raw material is low in cost, the process is simple, the reaction condition requirement is low, the safety is good, the product yield and purity are high, and the mass production is easy to realize. Moreover, the diester of a three-membered ring to an eighteen-membered ring can be prepared by utilizing the synthetic method of the invention.
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Paragraph 0025; 0026; 0027; 0028
(2018/11/03)
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- Synthesis, modelling, and μ-opioid receptor affinity of N-3(9)-arylpropenyl-N-9(3)-propionyl-3,9-diazabicyclo[3.3.1]nonanes
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A series of N-3-arylpropenyl-N-9-propionyl-3,9-diazabicyclo[3.3.1]nonanes (1a-g) and of reverted N-3-propionyl-N-9-arylpropenyl isomers (2a-g), as homologues of the previously reported analgesic 3,8-diazabicyclo[3.2.1]octanes (I-II), were synthesized and evaluated for the binding affinity towards opioid receptor subtypes μ, δ and κ. Compounds 1a-g and 2a-g exhibited a strong selective μ-affinity with Ki values in the nanomolar range, which favourably compared with those of I and II. In addition, contrary to the trend observed for DBO-I, II, the μ-affinity of series 2 is markedly higher than that of the isomeric series 1. This aspect was discussed on the basis of the conformational studies performed on DBN which allowed hypotheses on the mode of interaction of these compounds with the μ receptor.
- Pinna,Murineddu,Curzu,Villa,Vianello,Borea,Gessi,Toma,Colombo,Cignarella
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p. 553 - 562
(2007/10/03)
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- Conception et synthese de chelatants du fer III pour le traitement de la chlorose ferrique
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New iron chelates containing pyrocatechol subunits bounded in α-position of a linear dicarboxylic acid are reported.The design of the structure and the choice of the synthetic scheme (with the help of Assisted Organic Synthesis) are presented.The six steps synthesis scheduled, needs the protection-deprotection of the carboxylic acids and the use of gaiacol preferably to pyrochatecol.The synthetic route is discussed.The individual steps and the characteristics of 20 reaction intermediates and products are described.The scope of the study is presented.
- Mhenni, F.,Bouraoui, A.,Mighri, Z.,Gallo, R.
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p. 824 - 829
(2007/10/02)
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