603128-65-0

Upstream product

• 603128-64-9 (1R,2R)-2-(N-tert-butoxycarbonylamino)-cyclohexan-1-yl methanesulfonate 
• 24424-99-5 di-tert-butyl dicarbonate 
• 931-15-7 (1R,2R)-2-aminocyclohexanol 
• 115586-44-2 Butyric acid (1S,2S)-2-azido-cyclohexyl ester 
• 119479-49-1 (1S,2S)-trans-2-azidocyclohexanol 
• 155975-19-2 (1R,2R)-trans-2-(N-tert-butyloxycarbonyl)amino-1-cyclohexanol 
• 286-20-4 cyclohexane-1,2-epoxide 
• 110716-78-4 (1R,2R)-trans-2-azidocyclohexanol 
• 364385-54-6 (1S,2R)-2-tert-Butoxycarbonylamino-cyclohexylamine 

Downstream Products

• 1439908-17-4 (1R,2S)-2-azidocyclohexanamine hydrochloride 
• 603128-70-7 N-[(2R)-tert-butyloxycarbonylaminocyclohex-(1S)-yl]-N-(thymin-1-ylacetyl)glycine ethyl ester 
• 603128-68-3 N-[(2R)-tert-butyloxycarbonylaminocyclohex-(1S)-yl]-N-(chloroacetyl)glycine ethyl ester 
• 603128-66-1 N-[(2R)-tert-butyloxycarbonylaminocyclohex-(1S)-yl]glycine ethyl ester 
• 364385-54-6 (1S,2R)-2-tert-Butoxycarbonylamino-cyclohexylamine 

Relevant academic research and scientific papers

NOVEL NICOTINAMIDE DERIVATIVE OR SALT THEREOF

The object of the present invention is to provide a compound and a pharmaceutical composition having excellent Syk inhibitory activity. According to the present invention, a nicotinamide derivative represented by the following formula (I) or a salt thereof is provided, wherein R1 is a substituent represented by the following formula (II-1), (III-1), or (IV-1) (wherein R3, R4, R5, n, and X1 have the same definitions as those described in the specification), and R2 is a pyridyl, indazolyl, phenyl, pyrazolopyridyl, benzisoxazolyl, pyrimidinyl, or quinolyl group, each of which optionally has at least one substituent.

Helix-forming propensity of aliphatic urea oligomers incorporating noncanonical residue substitution patterns

Aliphatic N,N′-linked oligoureas are peptidomimetic foldamers that adopt a well-defined helical secondary structure stabilized by a collection of remote three-center H-bonds closing 12- and 14-membered pseudorings. Delineating the rules that govern helix formation depending on the nature of constituent units is of practical utility if one aims to utilize this helical fold to place side chains in a given arrangement and elaborate functional helices. In this work, we tested whether the helix geometry is compatible with alternative substitution patterns. The central -NH-CH(R)-CH2-NH-CO- residue in a model oligourea pentamer sequence was replaced by guest units bearing various substitution patterns [e.g., -NH-CH2-CH2-NH-CO-, -NH-CH2-CH(R)-NH-CO-, and -NH-CH(R1)-CH(R 2)-NH-CO-], levels of preorganization (cyclic vs acyclic residues), and stereochemistries, and the helix formation was systematically assessed. The extent of helix perturbation or stabilization was primarily monitored in solution by Fourier transform IR, NMR, and electronic circular dichroism spectroscopies. Our results indicate that although three new substitution patterns were accommodated in the 2.5-helix, the helical urea backbone in short oligomers is particularly sensitive to variations in the residue substitution pattern (position and stereochemistry). For example, the trans-1,2- diaminocyclohexane unit was experimentally found to break the helix nucleation, but the corresponding cis unit did not. Theoretical calculations helped to rationalize these results. The conformational preferences in this series of oligoureas were also studied at high resolution by X-ray structure analyses of a representative set of modified oligomers.

SELECTIVE KINASE INHIBITORS

Provided are pyrimidine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibition Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.

Novel Compounds

Compounds of Formulae I, or pharmaceutically acceptable salts thereof: wherein A1, A2, G1, G2 G3, R1, R2, X, Y, Z, m, n and p are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.

Microwave assisted fast and clean conversion of mesylate to azide: Synthesis of (1S,2R/1R,2S)-1-azido-2-carbocyclic amines as immediate precursors to versatile 1,2-cis-diamines

An efficient and rapid conversion of mesylate to azide under microwave irradiation has been carried out. It proceeds through inversion of configuration from chiral mesylates to provide optically pure cis-azides, immediate precursors of vicinal-cis-1,2-dia

Synthesis and Evaluation of (1S,2R/1R,2S)-Aminocyclohexylglycyl PNAs As Conformationally Preorganized PNA Analogues for DNA/RNA Recognition

Conformationally constrained cis-aminocyclohexylglycyl PNAs have been designed on the basis of stereospecific imposition of 1,2-cis-cyclohexyl moieties on the aminoethyl segment of aminoethylglycyl PNA (aegPNA). The introduction of the cis-cyclohexyl ring

(1S,2R/1R,2S)-aminocyclohexyl glycyl thymine PNA: Synthesis, monomer crystal structures, and DNA/RNA hybridization studies

(Matrix Presented) The synthesis of ethyl cis-(1s,2R/1R,2S)-2.aminocyclohex-1-yI-N-(thymin-1-yl-acetyl) glycinate (10a and 10b) via enzymatic resolution of the key racemic intermediate trans-2-azido cyclohexanols 3 is reported. The crystal structures of 10 show equatorial disposition of the tertiary amide group, with the torsion angle β in the range 60-70°. The PNA oligomers incorporating these show differential effects in hybridizing with complementary DNA and RNA.