97389-48-5Relevant academic research and scientific papers
Method for synthesizing medical intermediate (by machine translation)
-
Paragraph 0033; 0041-0050, (2020/07/15)
The synthesis method comprises the following steps: reacting SM1 and SM2 as starting materials to obtain the intermediate I; reacting the intermediate I obtained in one step with the benzyl bromide under the action of a reducing agent to generate the intermediate II of the formula (1); and the method has the advantages of high safety and environmental friendliness. (by machine translation)
HETEROARYL COMPOUNDS AS IRAK INHIBITORS AND USES THEREOF
-
Paragraph 00192, (2017/05/02)
The present invention relates to compounds of Formula (I) and pharmaceutically acceptable compositions thereof, useful as IRAK inhibitors.
4 -SUBSTITUTED BENZOXABOROLE COMPOUNDS AND USES THEREOF
-
Paragraph 00233, (2016/09/22)
Substituted benzoxaboroles whose structure comprises Formula (III), wherein R3 is selected from –CH3, –CH2CH3, –CH2=CH2, –CH2CH2CH3, –CH(CH3)sub
TRICYCLIC BENZOXABOROLE COMPOUNDS AND USES THEREOF
-
Paragraph 00260-00261, (2015/02/25)
Compounds of Formula II wherein X is selected from chloro, fluoro, bromo and iodo, R1 and R2 are each independently selected from H, -CH3, -CH2CH3, -CH2CH2CH3, or -CH(CH3)2
TRICYCLIC BORON COMPOUNDS FOR ANTIMICROBIAL THERAPY
-
Paragraph 0130; 0132; 0135; 0136, (2013/07/05)
Provided herein are antimicrobial tricyclic boron compounds of the following formula I: or pharmaceutically acceptable salts, complexes, or tautomers thereof that are antibacterial agents, pharmaceutical compositions containing them, methods for their use
Enantiocomplementary chemoenzymatic asymmetric synthesis of (R)- And (S)-chromanemethanol
Fuchs, Michael,Simeo, Yolanda,Ueberbacher, Barbara T.,Mautner, Barbara,Netscher, Thomas,Faber, Kurt
experimental part, p. 833 - 840 (2009/07/05)
A non-lipase-based, enantiocomplementary chemoenzymatic route towards enantiopure (R)- and (S)-chromane-methanol (12), which are the key building blocks for the synthesis of stereoisomerically pure α-tocopherols, has been achieved by the biocatalytic reso
Bacillus subtilis epoxide hydrolase-catalyzed preparation of enantiopure 2-methylpropane-1,2,3-triol monobenzyl ether and its application to expeditious synthesis of (R)-bicalutamide
Fujino, Aya,Asano, Masayoshi,Yamaguchi, Hitomi,Shirasaka, Naoki,Sakoda, Akiko,Ikunaka, Masaya,Obata, Rika,Nishiyama, Shigeru,Sugai, Takeshi
, p. 979 - 983 (2008/02/04)
Expeditious synthesis of (R)-bicalutamide (1), a synthetic antiandrogen, from enantiopure 2-methylpropane-1,2,3-triol monobenzyl ether (4) was achieved. An engineered Bacillus subtilis epoxide hydrolase worked enantioselectively on the racemic epoxide (7) to provide the above starting material in highly enantiomerically enriched state.
Chemo-enzymatic enantioconvergent synthesis of C4-building blocks containing a fully substituted chiral carbon center using bacterial epoxide hydrolases
Steinreiber,Hellstr?m,Mayer,Orru,Faber
, p. 111 - 113 (2007/10/03)
A highly efficient chemo-enzymatic asymmetric synthesis of chiral C4-building blocks containing a fully substituted carbon center is reported. The key transformation consists of a deracemization based on an enantioconvergent asymmetric hydrolys
Enantioselective hydrolysis of functionalized 2,2-disubstituted oxiranes with bacterial epoxide hydrolases
Steinreiber, Andreas,Osprian, Ingrid,Mayer, Sandra F.,Orru, Romano V. A.,Faber, Kurt
, p. 3703 - 3711 (2007/10/03)
The biohydrolysis of 2,2-disubstituted oxiranes bearing various oxygen functional groups was investigated using the epoxide hydrolase activity of 11 bacterial strains. The results show that the activity and the selectivity strongly depend on the substrate structure and the biocatalyst. Whereas substrates possessing free hydroxyl groups were not transformed, their analogs, protected as ethers, were well accepted. This allowed the convenient modulation of the enantioselectivity by proper choice of the ether group according to size and polarity. It was found that the distance of the ether-oxygen to the stereogenic quaternary carbon center of the oxirane ring had a profound influence on the enantioselectivity, and several oxiranes were resolved with good to excellent selectivities. The enantiomerically enriched epoxides and vicinal diols thus obtained contain a useful 'synthetic handle' in their side chain, which allows their use as building blocks in asymmetric synthesis.
Influence of a 2-fluoro substituent on diastereoselectivity in the 1,3-dipolar cycloadditions of nitrones
Ihara, Masataka,Tanaka, Yuko,Takahashi, Nobuyuki,Tokunaga, Yuji,Fukumoto, Keiichiro
, p. 3043 - 3052 (2007/10/03)
It is clear that the role of 1,2-asymmetric induction on the 1,3-dipolar cycloaddition of nitrones is influenced by the presence of a fluorine atom at the C-2 position. 2-Fluoro nitrones, synthesized by three different methods, have been subjected to the intermolecular 1,3-dipolar cycloaddition with ethyl vinyl ether. The stereostructures of isoxazolidines formed were determined by their conversion into 2,7-dioxa-6-azabicyclo[3.2.1]octanes. The diastereoselectivity of 2-fluoro nitrones was the reverse of that of the corresponding 2-hydro nitrones. This fact supports that the conformation with relief from the dipole repulsion between the fluorine atom and the oxygen atom of the nitrone is a preferred one for 2-fluoro nitrones, while the corresponding 2-hydro nitrones adopt the conformation with the least 1,3-allylic strain.
