134458-52-9

Upstream product

• 77943-39-6 4-methyl-5-phenyloxazolidin-2-one 
• 38136-29-7 4-methylvaleroyl chloride 
• 54418-69-8 4-methyl-5-phenyl-2-oxazolidinone 

Downstream Products

• 134458-66-5 3-<3(R)-<3-(tert-butyloxycarbonyl)-2,2-dimethyl-4(S)-isobutyl-5(R)-oxazolidinyl>-3-hydroxy-2(R)-isobutyl-1-oxopropyl>-4(R)-methyl-5(S)-phenyl-2-oxazolidinone 
• 877078-59-6 (4R,5S)-3-((S)-2-isobutylpent-4-enoyl)-4-methyl-5-phenyloxazolidin-2-one 
• 1345705-20-5 C₃₆H₄₅F₂N₃O₄ 
• 1345705-83-0 C₂₉H₃₈F₂N₄O₄ 
• 1345705-81-8 C₃₆H₄₄F₂N₄O₄ 
• 1345707-81-4 C₄₀H₆₀F₂N₄O₆Si 
• 1345706-43-5 C₄₇H₆₆F₂N₄O₆Si 
• 1345706-16-2 C₃₈H₆₃F₂N₃O₆Si 
• 1345706-06-0 C₄₅H₆₉F₂N₃O₆Si 
• 1345705-31-8 C₂₉H₃₉F₂N₃O₄ 

Relevant academic research and scientific papers

Total Synthesis of Leupyrrins A1 and B1, Highly Potent Antifungal Agents from the Myxobacterium Sorangium cellulosum

Full details on the design, elaboration, and application of efficient strategies for the high-yielding total syntheses of leupyrrins A1 and B1, unique antifungal agents from the myxobacterium Sorangium cellulosum, are reported. A sequential zirconocene-mediated diyne-cyclization, and regioselective opening of the zirconacyclopentadiene intermediate enabled a concise entry into the unique dihydrofuran fragment, whereas another domino reaction was developed for the butyrolactone involving a one-pot lactol opening, stereoselective aldehyde addition and in situ lactonization. Furthermore, an innovative sp2-sp3-cross-coupling for pyrrole functionalization and an optimized HATU-mediated amide coupling protocol of two elaborate fragments were established. In addition, an unusual protective group strategy, involving a Teoc-acetonide protected amine in combination with tert-butyl and acetate esters, was successfully elaborated. These tactics and strategies are generally useful and may be also applied in the synthesis of other functionalized compounds. It is expected that the material which was obtained by these total syntheses will enable the further exploration of the biological profile of these potent antifungal agents.

BETA-TETRAZOLYL-PROPIONIC ACIDS AS METALLO-BETA-LACTAMASE INHIBITORS

The present invention relates to compounds of formula I that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.

Monosubstituted γ-lactam and conformationally constrained 1,3-diaminopropan-2-ol transition-state isostere inhibitors of β-secretase (BACE)

The synthesis, evaluation, and structure-activity relationships of a class of γ-lactam 1,3-diaminopropan-2-ol transition-state isostere inhibitors of BACE are discussed. Two strategies for optimizing lead compound 1a are presented. Reducing the overall size of the inhibitors resulted in the identification of γ-lactam 1i, whereas the introduction of conformational constraint on the prime-side of the inhibitor generated compounds such as the 3-hydroxypyrrolidine inhibitor 28n. The full in vivo profile of 1i in rats and 28n in Tg 2576 mice is presented.

Novel gamma-lactams as beta-secretase inhibitors

There is provided a series of novel substituted gamma-lactams of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R4, R5 and R6 as defined herein, their ph

GABA and L-glutamic acid analogs for antiseizure treatment

A compound of the formula wherein R1is a straight or branched alkyl group having from 1 to 6 carbon atoms, phenyl, or cycloalkyl having from 3 to 6 carbon atoms; R2is hydrogen or methyl; and R3is hydrogen, methyl or carboxyl; which is useful in the treatment of seizure disorders. Processes are disclosed for the preparation of the compound. Intermediates prepared during the synthesis of the compound are also disclosed.

A modular synthetic approach toward exhaustively stereodiversified ligand libraries

(Matrix presented) This report describes a modular approach to the synthesis of stereodiversified natural product-like libraries. Monomers 2 and 3 were coupled in parallel by silyl-tethered olefin metathesis to generate all 16 stereoisomers of cis-enediol