156779-11-2Relevant articles and documents
ARYL, HETEROARY, AND HETEROCYCLIC PHARMACEUTICAL COMPOUNDS FOR TREATMENT OF MEDICAL DISORDERS
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Page/Page column 453; 454, (2018/09/21)
Complement Factor D inhibitors, pharmaceutical compositions, and uses thereof, as well as processes for their manufacture are provided. The compounds provided include Formula I, Formula II, Formula III, Formula IV, and Formula V, or a pharmaceutically acceptable salt, prodrug, isotopic analog, N-oxide, or isolated isomer thereof, optionally in a pharmaceutically acceptable composition. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade.
ANGIOTENSIN-(1-7) ANALOGS AND METHODS RELATING THERETO
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Paragraph 0143, (2017/07/06)
Angiotensin (1-7) analogs are provided. The analogs contain one or more substitutions with non-natural amino acid cis-3-(aminomethyl)cyclobutanecarboxylic acid (ACCA). Also provided are methods of making such analogs and methods for using such analogs as
Synthesis and reduction reactions of pyridones and 5-acyl-2-methoxypyridines
Bisset, Alexander A.,Dishington, Allan,Jones, Teyrnon,Clarkson, Guy J.,Wills, Martin
, p. 7207 - 7220 (2017/09/12)
The synthesis of a series of pyridones, from their 2-hydroxypyridine or 2-methoxypyridine precursors, is described, along with studies into their reductions to saturated heterocycles. A number of 5-acylpyridones were prepared and were evaluated as substrates for asymmetric transfer hydrogenation prior to conversion to saturated heterocycles. The enantioselective reduction of 5-acetyl-1-benzylpyrimidine-2,4(1H,3H)-dione is also described.
Synthesis of a conformationally constrained δ-amino acid building block
O'Reilly, Elaine,Pes, Lara,Ortin, Yannick,Mueller-Bunz, Helge,Paradisi, Francesca
, p. 511 - 518 (2013/07/27)
Conformationally restricted amino acids are important components in peptidomimetics and drug design. Herein, we describe the synthesis of a novel, non-proteinogenic constrained delta amino acid containing a cyclobutane ring, cis-3(aminomethyl)cyclobutane
An efficient synthetic route to functionalized δ-lactams
Samarat, Ali,Ben Kra?em, Jihène,Ben Ayed, Ta?cir,Amri, Hassen
, p. 9540 - 9543 (2008/12/22)
This paper describes a convenient synthesis of disubstituted functionalized δ-lactams based on Michael addition of primary amines to dimethyl-E-2-alkylidene glutarates 2 followed by an intramolecular cyclisation.
A flexible strategy for the synthesis of tri- and tetracyclic lupin alkaloids: Synthesis of (+)-cytisine, (±)-anagyrine, and (±)-thermopsine
Gray, Diane,Gallagher, Timothy
, p. 2419 - 2423 (2007/10/03)
(Chemical Equation Presented) Looping the lupin: A general synthetic strategy for the construction of the lupin alkaloids has been defined and involves sequential formation of the N1-C10 and C6-C7 bonds, which are common to compounds of this class of natu
A short synthesis of (±)-cytisine
Botuha, Candice,Galley, Carl M. S.,Gallagher, Timothy
, p. 1825 - 1826 (2007/10/03)
The synthesis of racemic cytisine 1 has been completed using (i) N-selective alkylation of 6-bromopyridone with bromide 6 and (ii) Pd(o) mediated intramolecular a-arylation of lactam 8 as key steps to achieve rapid assembly of the tricyclic core skeleton of the lupin alkaloids.
Construction of Hydroxylated Alkaloids (+/-)-Mannonolactam, (+/-)-Deoxymannojirimycin, and (+/-)-Prosopinine through Aza-Annulation
Cook, Gregory R.,Beholz, Lars G.,Stille, John R.
, p. 3575 - 3584 (2007/10/02)
The aza-annulation of β-enamino carbonyl substrates with acrylate derivatives provides an efficient and convenient route for the regioselective construction of δ-lactams.This two-step ring-forming sequence involved initial generation of the benzyl enamine through either a condensation or conjugate addition reaction with BnNH2, followed by aza-annulation with acryloyl chloride or acrylic anhydride.Controlled by the rigid framework of the intermediate lactam, introduction of ring substituents was accomplished with high relative stereoselectivity.The carbonyl functionality, which was necessary to direct the regioselectivity of the aza-annulation reaction, was then transformed into a protected hydroxyl substituent through Baeyer-Villiger oxidation.The resultant δ-lactam product was used as a valuable intermediate in the synthesis of three natural products.Subsequent modification of this δ-lactam gave the naturally occurring α-mannosidase inhibitors (+/-)-mannonolactam and (+/-)-deoxymannojirimycin, while synthesis of the alkaloid (+/-)-prosopinine was accomplished through homologation of the lactam carbonyl.
