34284-28-1Relevant articles and documents
Method for synthesizing Fimasartan
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Paragraph 0054; 0055; 0056, (2018/05/16)
The invention discloses a method for synthesizing Fimasartan. The method comprises the steps: subjecting a compound VI and a compound VII to a reaction in toluene, so as to obtain a compound V; subjecting the compound V and pentamidine hydrochloride to a reaction in the presence of alkali metal hydroxide, so as to obtain a compound IV; subjecting the compound IV to hydrogen drawing with lithium hydride in a mixed solvent prepared from toluene and DMF, and then, carrying out an N-alkylation reaction with 2-cyano-4'-bromo-methyl biphenyl, so as to obtain a compound III; subjecting the compound III and sodium azide to a reaction in DMF in the presence of zinc chloride, so as to obtain a compound II; and subjecting the compound II to a thio amidation reaction with a Lawesson's reagent, therebyobtaining the target product I. According to the method, the process is simple, the operation is simple and convenient, the raw materials are readily available, and the method is economical and efficient, so that the production cost of the Fimasartan is greatly reduced, and the industrial production is easy to achieve.
Achieving chemo-, regio-, and stereoselectivity in palladium-catalyzed reaction of γ-borylated allylic acetates
Kukkadapu, Krishna Kishore,Ouach, Aziz,Lozano, Pedro,Vaultier, Michel,Pucheault, Mathieu
supporting information; experimental part, p. 4132 - 4135 (2011/10/02)
Three-carbon highly functionalized γ-borylated allylic acetates underwent a regio- and stereocontrolled Tsuji-Trost reaction in the presence of palladium complexes. An ipso substitution of the acetate with complete stereoretention of the chiral center was achieved, leading to vinylic boronates with enantiomeric excesses above 99%.