51419-59-1Relevant articles and documents
Preparation method of novel abscisic acid agonist AM1
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Paragraph 0017; 0022, (2021/05/12)
The invention discloses a preparation method of a novel abscisic acid agonist AM1, and relates to chemical synthesis. The preparation method comprises the following steps: taking cheap quinoline as a raw material, and preparing a key intermediate 1-propyl
Alkyne Linchpin Strategy for Drug:Pharmacophore Conjugation: Experimental and Computational Realization of a Meta-Selective Inverse Sonogashira Coupling
Bhowmick, Suman,Guin, Srimanta,Kumar Singh, Vikas,Maiti, Debabrata,Paton, Robert S.,Porey, Sandip,Zhang, Xinglong
supporting information, p. 3762 - 3774 (2020/03/10)
The late-stage functionalization (LSF) of pharmaceutical and agrochemical compounds by the site-selective activation of C-H bonds provides access to diverse structural analogs and expands synthetically-accessible chemical space. We report a C-H functionalization LSF strategy that hinges on the use of an alkyne linchpin to assemble conjugates of sp2-rich marketed pharmaceuticals and agrochemicals with sp3-rich 3D fragments and natural products. This is accomplished through a template-assisted inverse Sonogashira reaction that displays high levels of selectivity for the meta position. This protocol is also amenable to distal structural modifications of α-amino acids. The transformation of alkyne functionality to other functional groups further highlights the applicative potential. Computational and experimental mechanistic studies shed light on the detailed mechanism. Turnover-limiting 1,2-migratory insertion of the bromoalkyne coupling partner occurs after relatively fast C-H activation. While this insertion occurs unselectively, regioconvergence results from one of the adducts undergoing a 1,2-trialkylsilyl migration to form the alkynylated product. A heterobimetallic Pd-Ag transition structure is essential for product formation in the β-bromide elimination step.
Method for rapidly preparing abscisic acid receptor stimulant
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Paragraph 0024, (2019/05/08)
The invention discloses a method for rapidly preparing an abscisic acid receptor stimulant and relates to a chemical synthesis and plant growing regulation technology. The method is characterized in that the two-step one-pot strategy is adopted, 4-methylb