- Total Synthesis of Penicibilaenes via C-C Activation-Enabled Skeleton Deconstruction and Desaturation Relay-Mediated C-H Functionalization
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Herein, we describe the first total synthesis of sesquiterpene penicibilaenes A and B through a "C-C/C-H"approach. In the "C-C"stage, the Rh-catalyzed "cut-and-sew"transformation between trisubstituted alkene and cyclobutanone has been employed to constru
- Xue, Yibin,Dong, Guangbin
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- Cyclobutenone as a highly reactive dienophile: Expanding upon diels-alder paradigms
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Cyclobutenone was employed as a dienophile in Diels-Alder cycloadditions, provide diverse and complex cycloadducts in good yields. Experimental outcomes indicated cyclobutenone to be more reactive than either cyclopentenone or cyclohexenone. In addition, cycloadducts bearing a strained cyclobutanone moiety were able to undergo regioselective ring expansions to produce corresponding cyclopentanones, lactones, and lactams, which are otherwise difficultly obtained by direct Diels-Alder reactions.
- Li, Xiaohua,Danishefsky, Samuel J.
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- Preparation method of 3-(benzyloxy)-1-cyclobutanone
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The invention relates to the technical field of organic synthesis, and specifically relates to synthesis of a medical intermediate 3-(benzyloxy)-1-cyclobutanone, according to the invention, 3-dibromo-2,3-dibromo-2,3,3-tetramethylpiperidine and diisopropyl malonate are used as initial raw materials; firstly, cyclobutane (I) is obtained through a nucleophilic substitution reaction; deprotection andhydrolysis are carried out on a compound (I) under the action of an acid to obtain 3-oxocyclobutanecarboxylic acid (II), the compound (II) is converted into a carboxylic acid silver salt, a Hunsdiecker reaction is carried out on the carboxylic acid silver salt and elemental bromine to obtain alkyl bromide (III), and a nucleophilic substitution reaction is performed on the compound (III) and benzylalcohol to obtain 3-(benzyloxy)-1-cyclobutanone (IV). The method provides a simple industrial production route for 3-(benzyloxy)-1-cyclobutanone, and has the advantages of simple reaction operation,mild reaction conditions and low cost.
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Paragraph 0049-0051
(2020/07/12)
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- Fused Bicyclic Kinase Inhibitors
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Compounds of Formula I, as shown below and defined herein: pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven at least in part by at least one of RON, MET or ALK. This Abstract is not limiting of the invention.
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Page/Page column 59
(2011/11/30)
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- KINASE INHIBITORS AND METHODS OF USE
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The present invention provides chemical entities or compounds and pharmaceutical compositions thereof that are capable of modulating certain protein kinases such as mTor, tyrosine kinases, and/or lipid kinases such as PI3 kinase. Also provided in the present invention are methods of using these compositions to modulate activities of one or more of these kinases, especially for therapeutic applications.
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Page/Page column 86-87
(2010/04/03)
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- AMINO PYRIMIDINE ANTICANCER COMPOUNDS
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Compounds of Formula (1), as shown below and defined herein: and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by FAK.
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Page/Page column 91
(2010/12/29)
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