245487-53-0

Upstream product

• 943-73-7 D-homophenylalanine 
• 60425-49-2 (+)-α-amino-4-phenylbutyric acid methyl ester hydrochloride 
• 74-89-5 methylamine 
• 82732-07-8 Boc-L-homophenylalanine 
• 110755-67-4 N-BOC-L-homophenylalanine-N-methylamide 

Downstream Products

• 1050311-00-6 (S)-methyl 2-{1-isobutyl-3-[1-(methylamino)-1-oxo-4-phenylbutan-2-yl]ureido}acetate 
• 1050311-03-9 (S)-methyl 2-{1-(cyclopropylmethyl)-3-[1-(methylamino)-1-oxo-4-phenylbutan-2-yl]ureido}acetate 
• 1050310-91-2 (S)-2-{3-(cyclopropylmethyl)-3-[2-(hydroxyamino)-2-oxoethyl]ureido}-N-methyl-4-phenylbutanamide 
• 1050310-89-8 (S)-2-{3-[2-(hydroxyamino)-2-oxoethyl]-3-isobutylureido}-N-methyl-4-phenylbutanamide 
• 1344706-29-1 (S)-2-((R/S)-2-hydroxy-2-(4-(5-(3-phenyl-4-(trifluoromethyl)isoxazol-5-yl)-1,2,4-oxadiazol-3-yl)phenyl)acetamido)-N-methyl-4-phenylbutanamide 
• 927828-21-5 (2R)-2-isobutyl-N₁-((S)-1-(methylamino)-1-oxo-4-phenylbutan-2-yl)-N₄-(tetrahydro-2H-pyran-2-yloxy)succinamide 
• 927828-23-7 (3R)-3-isobutyl-1-(tetrahydro-2H-pyran-2-yloxy)pyrrolidine-2,5-dione 
• 927828-22-6 (2R)-2-isobutyl-N₄-((S)-1-(methylamino)-1-oxo-4-phenylbutan-2-yl)-N₁-(tetrahydro-2H-pyran-2-yloxy)succinamide 
• 927828-11-3 (S)-methyl 4-methyl-2-(2-((S)-1-(methylamino)-1-oxo-4-phenylbutan-2-ylamino)-2-oxoethyl)pentanoate 
• 927828-17-9 (S)-tert-butyl 5-methyl-3-((S)-1-(methylamino)-1-oxo-4-phenylbutan-2-ylcarbamoyl)hexanoate 

Relevant academic research and scientific papers

Asymmetric and Geometry-Selective α-Alkenylation of α-Amino Acids

Both E- and Z-N′-alkenyl urea derivatives of imidazolidinones may be formed selectively from enantiopure α-amino acids. Generation of their enolate derivatives in the presence of K+ and [18]crown-6 induces intramolecular migration of the alkeny

Substituted Dihydroisoquinolinones by Iodide-Promoted Cyclocarbonylation of Aromatic α-Amino Acids

Imidazolidinone derivatives of a range of aromatic α-amino acids, on treatment with phosgene and potassium iodide, undergo a mild Bischler-Napieralski-style cyclocarbonylation reaction that generates a tricyclic lactam by insertion of a C=O group between amino acid nitrogen and the ortho position of the aryl substituent. Regio- and diastereoselective functionalization of the lactam generates a library of substituted dihydroisoquinolinones and their congeners in enantioenriched form.

Aromatic Interactions in Organocatalyst Design: Augmenting Selectivity Reversal in Iminium Ion Activation

Substituting N-methylpyrrole for N-methyindole in secondary-amine-catalysed Friedel-Crafts reactions leads to a curious erosion of enantioselectivity. In extreme cases, this substrate dependence can lead to an inversion in the sense of enantioinduction. Indeed, these closely similar transformations require two structurally distinct catalysts to obtain comparable selectivities. Herein a focussed molecular editing study is disclosed to illuminate the structural features responsible for this disparity, and thus identify lead catalyst structures to further exploit this selectivity reversal. Key to effective catalyst re-engineering was delineating the non-covalent interactions that manifest themselves in conformation. Herein we disclose preliminary validation that intermolecular aromatic (CH-π and cation-π) interactions between the incipient iminium cation and the indole ring system is key to rationalising selectivity reversal. This is absent in the N-methylpyrrole alkylation, thus forming the basis of two competing enantio-induction pathways. A simple L-valine catalyst has been developed that significantly augments this interaction.

UREA DERIVATIVES AND THEIR THERAPEUTIC USE

A compound of formula (I) wherein R1 is C1-6 alkyl optionally substituted by OH, C1-4 alkyl, SH, C1-4 alkylthio, phenyl or indol-3-yl, wherein C1-4 alkyl and C1-4 alkylthio are optionally s

Novel method of treatment of inflammatory skin conditions

There is provided, inter alia, a method for the treatment or prevention of an inflammatory skin condition which is characterised by colonisation with Staphylococcus aureus, comprising the topical administration of an aureolysin inhibitor.

USE OF AN AUREOLYSIN INHIBITOR FOR THE TREATMENT OF INFLAMMATORY SKIN CONDITIONS CHARACTERISED BY COLONISATION WITH STAPHYLOCOCCUS AUREUS

There is provided, inter alia, a method for the treatment or prevention of an inflammatory skin condition which is characterised by colonisation with Staphylococcus aureus, comprising the topical administration of an aureolysin inhibitor.

Synthesis and biological evaluation of orally active matrix metaloproteinase inhibitors

The synthesis and biological evaluation of orally active inhibitors of matrix metalloproteinase are reported. Modifications of the P2' position and the α-substituent of hydroxamic acid derivatives were carried out, and revealed that the P2' substituent influenced the MMP inhibitory activities in vitro and in plasma after oral administration. The hydroxamates with phenylglycine at the P2' position were absorbed well orally. Compound 15e, which exhibited the longest duration of inhibitory activity in plasma after oral administration among the phenylglycine derivatives (5a-5d, 15a, 15c, 15e), was evaluated in a rat adjuvant arthritis model. A reduction in hind foot pad swelling and improvements of some inflammatory parameters were demonstrated when the compound was administered orally. These results indicate the potential of MMP inhibitors for rheumatoid arthritis.