80662-83-5Relevant academic research and scientific papers
AZOCANE AND AZONANE DERIVATIVES AND METHODS OF TREATING HEPATITIS B INFECTIONS
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Paragraph 0317; 0318; 0319, (2016/10/11)
Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
Synthesis of an azabicyclic framework towards (±)-actinophyllic acid
Mortimer, Danny,Whiting, Matthew,Harrity, Joseph P.A.,Jones, Simon,Coldham, Iain
, p. 1255 - 1257 (2014/02/14)
Lewis acid mediated intramolecular Mannich reaction between an azocinone and a 3-formylindole was investigated as part of a study towards the synthesis of actinophyllic acid. The intramolecular Mannich reaction resulted in a single diastereomer of the 1-azabicyclo[4.2.1]nonan-5-one core framework, although single crystal X-ray structure analysis revealed that this had the undesired stereochemistry in comparison with the natural product.
Side chain SAR of bicyclic β-lactamase inhibitors (BLIs). 1. Discovery of a class C BLI for combination with imipinem
Blizzard, Timothy A.,Chen, Helen,Kim, Seongkon,Wu, Jane,Young, Katherine,Park, Young-Whan,Ogawa, Amy,Raghoobar, Susan,Painter, Ronald E.,Hairston, Nichelle,Lee, Sang Ho,Misura, Andrew,Felcetto, Tom,Fitzgerald, Paula,Sharma, Nandini,Lu, Jun,Ha, Sookhee,Hickey, Emily,Hermes, Jeff,Hammond, Milton L.
scheme or table, p. 918 - 921 (2010/08/06)
Bridged monobactam β-lactamase inhibitors were prepared and evaluated as potential partners for combination with imipenem to overcome class C β-lactamase mediated resistance. The (S)-azepine analog 2 was found to be effective in both in vitro and in vivo assays and was selected for preclinical development.
NOVEL INHIBITORS OF BETA-LACTAMASE
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Page/Page column 47, (2008/06/13)
A class of 7-oxo-2,6-diazabicyclo-[3.2.0]-heptane-6-sulfonic acid compounds substituted at the two position of the bicyclic ring with a heterocyclylaminocarbonyl group or a carbocyclylaminocarbonyl group are β-lactamase inhibitors. The compounds and their prodrugs and pharmaceutically acceptable salts are useful in the treatment of bacterial infections in combination with β-lactam antibiotics. In particular, the compounds are suitable for use with β-lactam antibiotics (e.g., imipenem and ceftazidime) against micro-organisms resistant to β-lactam antibiotics due to the presence of the β-lactamases.
Ring transformation of 1,2,3,5,6,7-hexahydropyrrolizinium perchlorates into 1-substituted 5-oxoperhydroazocines
Sumoto,Mibu,Irie,Abe,Miyano
, p. 577 - 580 (2007/10/02)
A facile ring transformation of 1,2,3,5,6,7-hexahydropyrrolizinium perchlorates (1 and 2) to 1-substituted 5-oxoperhydroazocines (5) is described. The spectroscopic and chemical properties of these products are also presented.
A NEW ROUTE TO 1-ACYL-5-OXOPERHYDROAZOCINE CORE USING 1,2,3,5,6,7-HEXAHYDROPYRROLIZINIUM PERCHLORATES
Miyano, Seiji,Mibu, Nobuko,Irie, Michiko,Sumoto, Kunihiro
, p. 2121 - 2126 (2007/10/02)
A convenient simple method for the synthesis of 1-substituted 5-oxoperhydroazocinea (1) is described.The method consists of N-acylation of 5-oxoperhydroazocine which is one of the tautomers of the pseudobase (3) generated by the treatment of 1,2,3,5,6,7-hexahydropyrrolizinium perchlorate with aqueous alkali.
Hydroboration-Carbon Monoxide Insertion of Bis-Olefinic Amine Derivatives. Synthesis of δ-Coniceine, Pyrrolizidine, (+/-)-Heliotridane, and (+/-)-Pseudoheliotridane
Garst, Michael E.,Bonfiglio, John N,Marks, Jeffrey
, p. 1494 - 1500 (2007/10/02)
The hydroboration-carbon monoxide insertion of several bis-olefinic derivatives has provided facile preparations of N-(carbomethoxy)-5-azacyclooctanone (6), N-(carbobenzyloxy)-5-azacyclooctanone (9), and N-(carbobenzyloxy)-5-cyclononanone (18).Of the hydroboration protocols examined, thexylborane-cyanidation proved to be the most useful.Reductive ring closure of 9 and of 18 gave 26 and 27, respectively.Methylation of 9 followed by reduction afforded 29 and 30.
