244075-39-6Relevant articles and documents
COMPOUNDS AND COMPOSITIONS USEFUL FOR TREATING DISORDERS RELATED TO NTRK
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Page/Page column 77, (2017/03/14)
This invention relates to inhibitors of NTRK that are active against wild-type NTRK and its resistant mutants.
Synthesis and fungistatic activity of bicyclic lactones and lactams against Botrytis cinerea, Penicillium citrinum, and Aspergillus glaucus
Walczak, Paulina,Pannek, Jakub,Boratyński, Filip,Janik-Polanowicz, Agata,Olejniczak, Teresa
, p. 8571 - 8578 (2014/11/07)
Six analogues of natural trans-4-butyl-cis-3-oxabicyclo[4.3.0]nonan-2-one (3) and three derivatives, 11, 12, and 13, of Vince lactam (10) were synthesized and tested as fungistatic agents against Botrytis cinerea AM235, Penicillium citrinum AM354, and six
Synthesis and Fungistatic Activity of Bicyclic Lactones and Lactams against Botrytis cinerea, Penicillium citrinum, and Aspergillus glaucus
Walczak, Paulina,Pannek, Jakub,Boratynski, Filip,Janik-Polanowicz, Agata,Olejniczak, Teresa
, p. 8571 - 8578 (2015/04/22)
Six analogues of natural trans-4-butyl-cis-3-oxabicyclo[4.3.0]nonan-2-one (3) and three derivatives, 11, 12, and 13, of Vince lactam (10) were synthesized and tested as fungistatic agents against Botrytis cinerea AM235, Penicillium citrinum AM354, and six strains of Aspergillus. Moreover, bioresolution carried out by means of whole cell microorganisms and commercially available enzymes afforded opposite enantiomerically enriched (a) and (+) isomers of Vince lactam (10), respectively. The effect of compound structures and stereogenic centers on biological activity has been discussed. The highest fungistatic activity was observed for four lactones: 3, 4, 7, and 8 (IC50 = 104.6-115.2 g/mL) toward B. cinerea AM235. cis-5,6-Epoxy-2-aza[2.2.1]heptan-3-one (13) indicated significant fungistatic activity (IC50 = 107.1 g/mL) against Aspergillus glaucus AM211. trans-4-Butyl-cis-3-oxabicyclo[4.3.0]nonan-2-one (3) and trans-4-butyl-cis-3-oxabicyclo[4.3.0]non-7-en-2-one (7) exhibited high fungistatic activity (IC50 = 143.2 and 110.2 g/mL, respectively) against P. citrinum AM354 as well.
Preparation of 2',3'-oxirane-fused carbocyclic nucleosides based on N-substituted 2-azabicyclo[2.2.1]-hept-5-en-3-ones
Ishikura, Minoru,Matsumoto, Kota,Murakami, Atsushi
, p. 241 - 248 (2007/10/03)
The epoxidation of N-substituted 2-azabicyclo[2.2.1]hept-5-en-3-ones (1) led to the exo-selective formation of epoxides (2), and the use of 2 for the preparation of 2',3'-oxirane-fused carbocyclic nucleosides (10) was attempted.
Highly selective directed hydrogenation of enantiopure 4-(tert-butoxycarbonylamino)cyclopent-1-enecarboxylic acid methyl esters
Smith, Mark E.B.,Derrien, Nadine,Lloyd, Michael C.,Taylor, Stephen J.C.,Chaplin, David A.,McCague, Raymond
, p. 1347 - 1350 (2007/10/03)
The use of both N-tert-butoxycarbonylamino- and hydroxyl-directed hydrogenation methodology to yield essentially single diastereomers of 3-(tert-butoxycarbonylamino)-4-hydroxycyclopentanecarboxylic acid methyl esters and 3-(tert-butoxycarbonylamino)cyclopentanecarboxylic acid methyl esters is described. These results incorporate the first reported carbamate-directed hydrogenations of functionalised cyclopentenes.
2-azabicyclo[2.2.1]hept-5-en-3-one epoxide: A versatile intermediate for the synthesis of cyclopentyl carbocyclic 2-deoxy-, 3-deoxy- and ara- ribonucleoside analogues.
Dominguez, Belen M.,Cullis, Paul M.
, p. 5783 - 5786 (2007/10/03)
5,6-Epoxy-exo-2-azabicyclo[2.2.1]heptan-3-one has been used as a versatile intermediate in the synthesis of 2-deoxy-, 3-deoxy- and ara- cyclopentyl carbocyclic nucleosides. An efficient, short synthesis of the (+) carbocyclic thymidine 13 is reported.
Synthesis of nucleosides and related compounds. XXII. Carbocyclic analogues of thymidine and related compounds from 2-azabicyclo[2.2.1]hept-5-en-3-ones
Katagiri,Nomura,Muto,Kaneko
, p. 1682 - 1688 (2007/10/02)
Reductive amido bond cleavage reaction, previously elaborated by our laboratory for the synthesis of carbocyclic ribothymidine from readily available 2-azabicyclo[2.2.1]hept-5-en-3-one, was successfully applied to the synthesis of carbocyclic analogues of thymidine and related compounds.
Epoxidation of 2-Azabicyclohept-5-en-3-one
Legraverend, Michel,Bisagni, Emile,Huel, Christiane
, p. 1881 (2007/10/02)
Epoxidation of 2-azabicyclohept-5-en-3-one has been performed in high yield with potassium hydrogen persulfate at pH 6, 1H nmr data indicate an exo stereoconfiguration of the epoxide.
