- Iprodione synthetic method
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The invention discloses an iprodione synthetic method, aiming to solve the technical problems of low content and environmental pollution of products prepared by the prior art. The iprodione syntheticmethod includes adding organic solvent and triphosgene in a reaction flask, adding organic solvent mixed solution of 3,5-dichloroaniline and catalysts dropwise at the temperature of 0-50 DEG C, afterthat, rising the temperature for the first time to 60-90 DEG C and then reacting for 2-6 hours, further, rising the temperature for the second time to 100-140 DEG C after finishing the reaction, and then reacting for 4-8 hours. Triphosgene and 3,5-dichloroaniline are reacted to obtain an intermediate I, namely 3,5-dichlorophenyl isocyanate, and then to obtain an intermediate II by means of condensation and acidification; the intermediate II is then subjected to cyclization to obtain an intermediate III; thus, iprodione synthesis is achieved directly without the process of separation. The iprodione synthetic method has the advantages of mild condition, high yield and less side reaction; the yield can be 83% by four steps.
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Paragraph 0014; 0016-0027
(2018/07/30)
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- Second grade chromene penicillin sodium pharmaceutical intermediate 2 - ethoxy group naphthalene formic acid (by machine translation)
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Abstract The present invention discloses naproxen sodium drug intermediates 2-ethoxynaphthaloic acid synthesis method by 3 -(1 -hydroxy-2-chloroethane) 5 -4-ethoxy naphthol solution and ethylene glycol monobenzyl ether were added to the reaction vessel, stirred, added nickel fluoride, raised the temperature of the solution, continued to react; added potassium sulfate solution, washed with chloropropane solution, washed with the chlorinated naphthalene solution, added the trifluoroacetic acid solution to adjust the pH, precipitated the solid, filtered, the solid recrystallizated 10 in the chloroform solution, dehydrated with dehydration, got the finished product 2-ethoxy naphthoic acid.
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Paragraph 0014; 0016-0027
(2018/07/30)
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- Frozen Chirality of Tertiary Aromatic Amides: Access to Enantioenriched Tertiary α-Amino Acid or Amino Alcohol without Chiral Reagent
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One of the fundamental and intriguing aspects of life is the homochirality of the essential molecules. In this field, the absolute asymmetric synthesis of α-amino acids is a major challenge. Herein, we report access, by chemical means, to tertiary α-amino acid derivatives in up to 96 % ee without using any chiral reagent. In our strategy, the dynamic axial chirality of tertiary aromatic amides is frozen in a crystal and is responsible for the stereoselectivity of the subsequent steps. Furthermore, we could control the configuration of the final product by manually sorting and selecting the initial crystals. Based on vibrational circular dichroism studies, we could rationalize the observed stereoselectivity.
- Mai, Thi Thoa,Viswambharan, Baby,Gori, Didier,Guillot, Régis,Naubron, Jean-Valère,Kouklovsky, Cyrille,Alezra, Valérie
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supporting information
p. 5787 - 5798
(2017/04/28)
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