Br?nsted Acid-Catalyzed Aza-Ferrier Reaction of N, O-Allenyl Acetals: Synthesis of β-Amino-α-methylene Aldehydes
A Tf2NH-catalyzed aza-Ferrier reaction of N,O-allenyl acetals was reported. This protocol provided various types of β-amino-α-methylene aldehydes as the products. The N,O-allenyl acetal substrates were easily prepared by base-induced isomerization of N,O-propargyl acetals with Triton B. The N,O-propargyl acetals were prepared from the corresponding aldehydes or lactams. Further synthetic applications of the products were also described.
Modular synthesis of the pentacyclic core of batrachotoxin and select batrachotoxin analogue designs
Pentacyclic analogues of the potent voltage-gated sodium ion channel agonist batrachotoxin can be accessed through an intermediate furan by exploiting Diels-Alder cycloaddition reactions with ring-strained dienophiles. The use of 3-bromofuran as a 1,2-dianion equivalent, the application of carbamate reductive N-alkylation for homomorpholine ring assembly, and the demonstration of CsF as an effective reagent for generating benzyne, cyclohexyne, and related dienophiles underscore this work.
Batrachotoxin Analogues, Compositions, Uses, and Preparation Thereof
Compounds relating to batrachotoxin are provided, in particular analogues that modulate the activity of sodium channels. Also provided are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier, includi
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Paragraph 0209; 0222-0223
(2014/06/25)
A short formal synthesis of three epimers of penmacric acid
An extremely short formal synthesis of three epimers of penmacric acid is accomplished starting from pyroglutamate in one or two steps. Stereochemical outcome in the reaction of Li and Ti enolates of pyroglutamate with imines is found to be dependent on both chelation and steric factors.
Sikriwal, Dimpy,Kant, Ruchir,Maulik, Prakas R.,Dikshit, Dinesh K.
experimental part
p. 6167 - 6173
(2010/10/02)
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